Chemicals
Showing 37051–37200 of 41137 results
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The peroxisome proliferator-activated receptor-γ (PPARγ) is the nuclear receptor responsible for transducing the therapeutic activity of the thiazolidinediones (TZDs). TZDs are a group of structurally related synthetic PPARγ receptor agonists with antidiabetic actions in vivo.{7575,8930} There are many PPARγ agonists, including 15-deoxy-Δ12,14-prostaglandin J2 and azelaoyl PAF, which are naturally derived.{8953,8224} However, only a few antagonists have been reported.{8241} T0070907 is a potent and selective antagonist of the human PPARγ with an apparent IC50 of 1 nM for the binding inhibition of rosiglitazone, a reference TZD. T0070907 covalently binds to Cys313 of PPARγ, inducing conformational changes that block the recruitment of transcriptional cofactors to the PPARγ/RXR heterodimer.{10311}
Brand:CaymanSKU:10026 - 50 mgAvailable on backorder
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The Liver X Receptors (LXRα and LXRβ) are nuclear hormone receptors whose native ligands are oxysterols, such as 22(R)-hydroxycholesterol. The LXRs regulate the oxysterol-induced expression of cholesterol 7α-hydroxylase, the rate limiting enzyme of classic bile acid synthesis. T0901317 is a potent and selective agonist for both LXRα and LXRβ, with an EC50 of about 50 nM.{8532} T0901317 acting through LXR and in concert with its RXR heterodimerization partner induces the expression of the ABCA1 reverse cholesterol transporter. This acts to increase the efflux of cholesterol from enterocytes and thus inhibit the overall absorption of cholesterol.
Brand:CaymanSKU:71810 - 10 mgAvailable on backorder
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The Liver X Receptors (LXRα and LXRβ) are nuclear hormone receptors whose native ligands are oxysterols, such as 22(R)-hydroxycholesterol. The LXRs regulate the oxysterol-induced expression of cholesterol 7α-hydroxylase, the rate limiting enzyme of classic bile acid synthesis. T0901317 is a potent and selective agonist for both LXRα and LXRβ, with an EC50 of about 50 nM.{8532} T0901317 acting through LXR and in concert with its RXR heterodimerization partner induces the expression of the ABCA1 reverse cholesterol transporter. This acts to increase the efflux of cholesterol from enterocytes and thus inhibit the overall absorption of cholesterol.
Brand:CaymanSKU:71810 - 100 mgAvailable on backorder
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The Liver X Receptors (LXRα and LXRβ) are nuclear hormone receptors whose native ligands are oxysterols, such as 22(R)-hydroxycholesterol. The LXRs regulate the oxysterol-induced expression of cholesterol 7α-hydroxylase, the rate limiting enzyme of classic bile acid synthesis. T0901317 is a potent and selective agonist for both LXRα and LXRβ, with an EC50 of about 50 nM.{8532} T0901317 acting through LXR and in concert with its RXR heterodimerization partner induces the expression of the ABCA1 reverse cholesterol transporter. This acts to increase the efflux of cholesterol from enterocytes and thus inhibit the overall absorption of cholesterol.
Brand:CaymanSKU:71810 - 50 mgAvailable on backorder
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Transmembrane protein 16A (TMEM16A, also known as anoctamin-1) is a calcium-activated chloride channel (CaCC) with roles in transepithelial anion transport and smooth muscle contraction. T16A(inh)-A01 is an aminophenylthiazole that inhibits transient TMEM16A-mediated chloride currents with an IC50 value of ~1 µM.{29772,29768} Its inhibitory effects are independent of voltage and do not prolong the rate of TMEM16A current deactivation.{29768} T16A(inh)-A01 blocks CaCC activity in vascular smooth muscle cells and relaxes mouse and human blood vessels.{29769} It also inhibits the proliferation of pancreatic cancer and squamous carcinoma cells in culture.{29771,29770}
Brand:CaymanSKU:-Available on backorder
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Transmembrane protein 16A (TMEM16A, also known as anoctamin-1) is a calcium-activated chloride channel (CaCC) with roles in transepithelial anion transport and smooth muscle contraction. T16A(inh)-A01 is an aminophenylthiazole that inhibits transient TMEM16A-mediated chloride currents with an IC50 value of ~1 µM.{29772,29768} Its inhibitory effects are independent of voltage and do not prolong the rate of TMEM16A current deactivation.{29768} T16A(inh)-A01 blocks CaCC activity in vascular smooth muscle cells and relaxes mouse and human blood vessels.{29769} It also inhibits the proliferation of pancreatic cancer and squamous carcinoma cells in culture.{29771,29770}
Brand:CaymanSKU:-Available on backorder
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Transmembrane protein 16A (TMEM16A, also known as anoctamin-1) is a calcium-activated chloride channel (CaCC) with roles in transepithelial anion transport and smooth muscle contraction. T16A(inh)-A01 is an aminophenylthiazole that inhibits transient TMEM16A-mediated chloride currents with an IC50 value of ~1 µM.{29772,29768} Its inhibitory effects are independent of voltage and do not prolong the rate of TMEM16A current deactivation.{29768} T16A(inh)-A01 blocks CaCC activity in vascular smooth muscle cells and relaxes mouse and human blood vessels.{29769} It also inhibits the proliferation of pancreatic cancer and squamous carcinoma cells in culture.{29771,29770}
Brand:CaymanSKU:-Available on backorder
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T5601640 is an inhibitor of LIM kinase 2 (LIMK2) that inhibits LIMK2-mediated cofilin phosphorylation.{41239} It reduces the levels of phosphorylated cofilin (p-cofilin) in mouse embryonic fibroblasts (MEF) lacking neurofibromin (Nf1-/-; IC50 = 30 µM), which normally have high levels of p-cofilin. T5601640 (50 µM) decreases actin stress fiber formation, inhibits cell migration, and inhibits colony formation of Nf1-/- MEF cells. It inhibits proliferation of ST88-14, U87, and PANC-1 cells with IC50 values of 18.3, 7.4, and 35.2 µM, respectively, and also decreases p-cofilin levels by 20, 24, and 46%, respectively.{41240} Oral gavage administration of T5601640 (60 mg/kg) decreases tumor volume and cofilin phosphorylation in a PANC-1 nude mouse xenograft model.
Brand:CaymanSKU:22140 -Out of stock
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T5601640 is an inhibitor of LIM kinase 2 (LIMK2) that inhibits LIMK2-mediated cofilin phosphorylation.{41239} It reduces the levels of phosphorylated cofilin (p-cofilin) in mouse embryonic fibroblasts (MEF) lacking neurofibromin (Nf1-/-; IC50 = 30 µM), which normally have high levels of p-cofilin. T5601640 (50 µM) decreases actin stress fiber formation, inhibits cell migration, and inhibits colony formation of Nf1-/- MEF cells. It inhibits proliferation of ST88-14, U87, and PANC-1 cells with IC50 values of 18.3, 7.4, and 35.2 µM, respectively, and also decreases p-cofilin levels by 20, 24, and 46%, respectively.{41240} Oral gavage administration of T5601640 (60 mg/kg) decreases tumor volume and cofilin phosphorylation in a PANC-1 nude mouse xenograft model.
Brand:CaymanSKU:22140 -Out of stock
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T5601640 is an inhibitor of LIM kinase 2 (LIMK2) that inhibits LIMK2-mediated cofilin phosphorylation.{41239} It reduces the levels of phosphorylated cofilin (p-cofilin) in mouse embryonic fibroblasts (MEF) lacking neurofibromin (Nf1-/-; IC50 = 30 µM), which normally have high levels of p-cofilin. T5601640 (50 µM) decreases actin stress fiber formation, inhibits cell migration, and inhibits colony formation of Nf1-/- MEF cells. It inhibits proliferation of ST88-14, U87, and PANC-1 cells with IC50 values of 18.3, 7.4, and 35.2 µM, respectively, and also decreases p-cofilin levels by 20, 24, and 46%, respectively.{41240} Oral gavage administration of T5601640 (60 mg/kg) decreases tumor volume and cofilin phosphorylation in a PANC-1 nude mouse xenograft model.
Brand:CaymanSKU:22140 -Out of stock
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T5601640 is an inhibitor of LIM kinase 2 (LIMK2) that inhibits LIMK2-mediated cofilin phosphorylation.{41239} It reduces the levels of phosphorylated cofilin (p-cofilin) in mouse embryonic fibroblasts (MEF) lacking neurofibromin (Nf1-/-; IC50 = 30 µM), which normally have high levels of p-cofilin. T5601640 (50 µM) decreases actin stress fiber formation, inhibits cell migration, and inhibits colony formation of Nf1-/- MEF cells. It inhibits proliferation of ST88-14, U87, and PANC-1 cells with IC50 values of 18.3, 7.4, and 35.2 µM, respectively, and also decreases p-cofilin levels by 20, 24, and 46%, respectively.{41240} Oral gavage administration of T5601640 (60 mg/kg) decreases tumor volume and cofilin phosphorylation in a PANC-1 nude mouse xenograft model.
Brand:CaymanSKU:22140 -Out of stock
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TA-01 is a derivative of the p38 MAPK inhibitor SB 203580 (Item Nos. 13067 | 13344) and an inducer of cardiomyocyte differentiation.{41744} It is cardiomyogenic at concentrations less than 5 μM, increasing expression of the cardiomyocyte marker NKX2-5 by 2.2-fold and decreasing expression of mesoderm markers and the pre-cardiac marker Isl-1 in HES-3 NKX2-5eGFP/w cells when applied after embryoid body formation. TA-01 inhibits casein kinase 1ε (CK1ε) and CK1Δ and reduces expression of Wnt/β-catenin signaling pathway members, activities that positively correlate with its cardiomyogenic activity.
Brand:CaymanSKU:24667 - 1 mgAvailable on backorder
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TA-01 is a derivative of the p38 MAPK inhibitor SB 203580 (Item Nos. 13067 | 13344) and an inducer of cardiomyocyte differentiation.{41744} It is cardiomyogenic at concentrations less than 5 μM, increasing expression of the cardiomyocyte marker NKX2-5 by 2.2-fold and decreasing expression of mesoderm markers and the pre-cardiac marker Isl-1 in HES-3 NKX2-5eGFP/w cells when applied after embryoid body formation. TA-01 inhibits casein kinase 1ε (CK1ε) and CK1Δ and reduces expression of Wnt/β-catenin signaling pathway members, activities that positively correlate with its cardiomyogenic activity.
Brand:CaymanSKU:24667 - 10 mgAvailable on backorder
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TA-01 is a derivative of the p38 MAPK inhibitor SB 203580 (Item Nos. 13067 | 13344) and an inducer of cardiomyocyte differentiation.{41744} It is cardiomyogenic at concentrations less than 5 μM, increasing expression of the cardiomyocyte marker NKX2-5 by 2.2-fold and decreasing expression of mesoderm markers and the pre-cardiac marker Isl-1 in HES-3 NKX2-5eGFP/w cells when applied after embryoid body formation. TA-01 inhibits casein kinase 1ε (CK1ε) and CK1Δ and reduces expression of Wnt/β-catenin signaling pathway members, activities that positively correlate with its cardiomyogenic activity.
Brand:CaymanSKU:24667 - 25 mgAvailable on backorder
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TA-01 is a derivative of the p38 MAPK inhibitor SB 203580 (Item Nos. 13067 | 13344) and an inducer of cardiomyocyte differentiation.{41744} It is cardiomyogenic at concentrations less than 5 μM, increasing expression of the cardiomyocyte marker NKX2-5 by 2.2-fold and decreasing expression of mesoderm markers and the pre-cardiac marker Isl-1 in HES-3 NKX2-5eGFP/w cells when applied after embryoid body formation. TA-01 inhibits casein kinase 1ε (CK1ε) and CK1Δ and reduces expression of Wnt/β-catenin signaling pathway members, activities that positively correlate with its cardiomyogenic activity.
Brand:CaymanSKU:24667 - 5 mgAvailable on backorder
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TA-02 is a derivative of the p38 MAPK inhibitor SB 203580 (Item Nos. 13067 | 13344) and an inducer of cardiomyocyte differentiation.{41744} It is cardiomyogenic, increasing expression of the cardiomyocyte marker NKX2-5 by greater than 2-fold and decreasing expression of mesoderm markers and the pre-cardiac marker Isl-1 in HES-3 NKX2-5eGFP/w cells when applied after embryoid body formation at a concentration of 5 μM. TA-02 inhibits casein kinase 1ε (CK1ε) and CK1D and reduces expression of Wnt/β-catenin signaling pathway members, activities that positively correlate with its cardiomyogenic activity.
Brand:CaymanSKU:24668 - 10 mgAvailable on backorder
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TA-02 is a derivative of the p38 MAPK inhibitor SB 203580 (Item Nos. 13067 | 13344) and an inducer of cardiomyocyte differentiation.{41744} It is cardiomyogenic, increasing expression of the cardiomyocyte marker NKX2-5 by greater than 2-fold and decreasing expression of mesoderm markers and the pre-cardiac marker Isl-1 in HES-3 NKX2-5eGFP/w cells when applied after embryoid body formation at a concentration of 5 μM. TA-02 inhibits casein kinase 1ε (CK1ε) and CK1D and reduces expression of Wnt/β-catenin signaling pathway members, activities that positively correlate with its cardiomyogenic activity.
Brand:CaymanSKU:24668 - 25 mgAvailable on backorder
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TA-02 is a derivative of the p38 MAPK inhibitor SB 203580 (Item Nos. 13067 | 13344) and an inducer of cardiomyocyte differentiation.{41744} It is cardiomyogenic, increasing expression of the cardiomyocyte marker NKX2-5 by greater than 2-fold and decreasing expression of mesoderm markers and the pre-cardiac marker Isl-1 in HES-3 NKX2-5eGFP/w cells when applied after embryoid body formation at a concentration of 5 μM. TA-02 inhibits casein kinase 1ε (CK1ε) and CK1D and reduces expression of Wnt/β-catenin signaling pathway members, activities that positively correlate with its cardiomyogenic activity.
Brand:CaymanSKU:24668 - 5 mgAvailable on backorder
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Tabersonine is an indole alkaloid that has been found in the beans of Voacanga.{43901} It inhibits amyloid-β (1-42) (Aβ42) fibril formation and disintegrates preformed Aβ42 fibrils in vitro when used at a concentration of 10 μM. Tabersonine is an intermediate in the biosynthesis of vindoline, a precursor in the synthesis of anticancer agents.{43907}
Brand:CaymanSKU:26848 - 1 mgAvailable on backorder
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Tabersonine is an indole alkaloid that has been found in the beans of Voacanga.{43901} It inhibits amyloid-β (1-42) (Aβ42) fibril formation and disintegrates preformed Aβ42 fibrils in vitro when used at a concentration of 10 μM. Tabersonine is an intermediate in the biosynthesis of vindoline, a precursor in the synthesis of anticancer agents.{43907}
Brand:CaymanSKU:26848 - 10 mgAvailable on backorder
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Tabersonine is an indole alkaloid that has been found in the beans of Voacanga.{43901} It inhibits amyloid-β (1-42) (Aβ42) fibril formation and disintegrates preformed Aβ42 fibrils in vitro when used at a concentration of 10 μM. Tabersonine is an intermediate in the biosynthesis of vindoline, a precursor in the synthesis of anticancer agents.{43907}
Brand:CaymanSKU:26848 - 25 mgAvailable on backorder
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Tabersonine is an indole alkaloid that has been found in the beans of Voacanga.{43901} It inhibits amyloid-β (1-42) (Aβ42) fibril formation and disintegrates preformed Aβ42 fibrils in vitro when used at a concentration of 10 μM. Tabersonine is an intermediate in the biosynthesis of vindoline, a precursor in the synthesis of anticancer agents.{43907}
Brand:CaymanSKU:26848 - 5 mgAvailable on backorder
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Tacrine is a derivative of aminoacridine that functions as an inhibitor of both acetylcholinesterase (AChE) and butyrylcholinesterase (IC50s = 31 and 26.5 nM, respectively).{6599,39197} Tacrine also inhibits the uptake of serotonin and norepinephrine in rat cerebral cortex and decreases depolarization-induced calcium influx through L-type calcium channels in SN56 neuronal cells.{4666,6602,6598} Formulations containing tacrine have been used clinically in the treatment of Alzheimer’s disease.{4666,6603}
Brand:CaymanSKU:70240 - 1 gAvailable on backorder
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Tacrine is a derivative of aminoacridine that functions as an inhibitor of both acetylcholinesterase (AChE) and butyrylcholinesterase (IC50s = 31 and 26.5 nM, respectively).{6599,39197} Tacrine also inhibits the uptake of serotonin and norepinephrine in rat cerebral cortex and decreases depolarization-induced calcium influx through L-type calcium channels in SN56 neuronal cells.{4666,6602,6598} Formulations containing tacrine have been used clinically in the treatment of Alzheimer’s disease.{4666,6603}
Brand:CaymanSKU:70240 - 5 gAvailable on backorder
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Tadalafil is a potent inhibitor of phosphodiesterase 5 (PDE5; IC50 = 1.2 nM).{24530} It is selective for PDE5 over PDE1-4 and 7-10 (IC50s = 9.2-280 μM), however, it does also inhibit PDE11 (IC50 = 11 nM). In vivo, tadalafil (10 mg/kg) decreases production of the proinflammatory cytokines TNF-α, IL-1β, and IL-6 and improves renal function in a rat model of ischemia/reperfusion injury.{41848} It also reduces development of tobacco smoke-induced emphysema and pulmonary hypertension in mice.{41849} Formulations containing tadalafil have been used to treat erectile dysfunction, pulmonary arterial hypertension, and lower urinary tract dysfunction.
Brand:CaymanSKU:- -
Tadalafil is a potent inhibitor of phosphodiesterase 5 (PDE5; IC50 = 1.2 nM).{24530} It is selective for PDE5 over PDE1-4 and 7-10 (IC50s = 9.2-280 μM), however, it does also inhibit PDE11 (IC50 = 11 nM). In vivo, tadalafil (10 mg/kg) decreases production of the proinflammatory cytokines TNF-α, IL-1β, and IL-6 and improves renal function in a rat model of ischemia/reperfusion injury.{41848} It also reduces development of tobacco smoke-induced emphysema and pulmonary hypertension in mice.{41849} Formulations containing tadalafil have been used to treat erectile dysfunction, pulmonary arterial hypertension, and lower urinary tract dysfunction.
Brand:CaymanSKU:- -
Tadalafil is a potent inhibitor of phosphodiesterase 5 (PDE5; IC50 = 1.2 nM).{24530} It is selective for PDE5 over PDE1-4 and 7-10 (IC50s = 9.2-280 μM), however, it does also inhibit PDE11 (IC50 = 11 nM). In vivo, tadalafil (10 mg/kg) decreases production of the proinflammatory cytokines TNF-α, IL-1β, and IL-6 and improves renal function in a rat model of ischemia/reperfusion injury.{41848} It also reduces development of tobacco smoke-induced emphysema and pulmonary hypertension in mice.{41849} Formulations containing tadalafil have been used to treat erectile dysfunction, pulmonary arterial hypertension, and lower urinary tract dysfunction.
Brand:CaymanSKU:- -
Tadalafil is a potent inhibitor of phosphodiesterase 5 (PDE5; IC50 = 1.2 nM).{24530} It is selective for PDE5 over PDE1-4 and 7-10 (IC50s = 9.2-280 μM), however, it does also inhibit PDE11 (IC50 = 11 nM). In vivo, tadalafil (10 mg/kg) decreases production of the proinflammatory cytokines TNF-α, IL-1β, and IL-6 and improves renal function in a rat model of ischemia/reperfusion injury.{41848} It also reduces development of tobacco smoke-induced emphysema and pulmonary hypertension in mice.{41849} Formulations containing tadalafil have been used to treat erectile dysfunction, pulmonary arterial hypertension, and lower urinary tract dysfunction.
Brand:CaymanSKU:- -
Tadalafil-d3 is intended for use as an internal standard for the quantification of tadalafil (Item No. 14024) by GC- or LC-MS. Tadalafil is a potent inhibitor of phosphodiesterase 5 (PDE5; IC50 = 1.2 nM).{24530} It is selective for PDE5 over PDE1-4 and 7-10 (IC50s = 9.2-280 μM), however, it does also inhibit PDE11 (IC50 = 11 nM). In vivo, tadalafil (10 mg/kg) decreases production of the proinflammatory cytokines TNF-α, IL-1β, and IL-6 and improves renal function in a rat model of ischemia/reperfusion injury.{41848} It also reduces development of tobacco smoke-induced emphysema and pulmonary hypertension in mice.{41849} Formulations containing tadalafil have been used to treat erectile dysfunction, pulmonary arterial hypertension, and lower urinary tract dysfunction.
Brand:CaymanSKU:25030 - 1 mgAvailable on backorder
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Tadalafil-d3 is intended for use as an internal standard for the quantification of tadalafil (Item No. 14024) by GC- or LC-MS. Tadalafil is a potent inhibitor of phosphodiesterase 5 (PDE5; IC50 = 1.2 nM).{24530} It is selective for PDE5 over PDE1-4 and 7-10 (IC50s = 9.2-280 μM), however, it does also inhibit PDE11 (IC50 = 11 nM). In vivo, tadalafil (10 mg/kg) decreases production of the proinflammatory cytokines TNF-α, IL-1β, and IL-6 and improves renal function in a rat model of ischemia/reperfusion injury.{41848} It also reduces development of tobacco smoke-induced emphysema and pulmonary hypertension in mice.{41849} Formulations containing tadalafil have been used to treat erectile dysfunction, pulmonary arterial hypertension, and lower urinary tract dysfunction.
Brand:CaymanSKU:25030 - 5 mgAvailable on backorder
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TAE-1 is a sym-triazine with diverse biological activities.{53142} It inhibits in vitro amyloid-β (1-42) (Aβ42; Item No. 20574) fibrilization when used at a concentration of 20 µM. TAE-1 inhibits acetylcholinesterase (AChE; IC50 = 0.465 µM for the human erythrocyte enzyme). It also increases neuronal cellular process length and branching and synaptophysin protein levels in differentiated human SH-SY5Y neuronal cells.
Brand:CaymanSKU:20464 -Available on backorder
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TAE-1 is a sym-triazine with diverse biological activities.{53142} It inhibits in vitro amyloid-β (1-42) (Aβ42; Item No. 20574) fibrilization when used at a concentration of 20 µM. TAE-1 inhibits acetylcholinesterase (AChE; IC50 = 0.465 µM for the human erythrocyte enzyme). It also increases neuronal cellular process length and branching and synaptophysin protein levels in differentiated human SH-SY5Y neuronal cells.
Brand:CaymanSKU:20464 -Available on backorder
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TAE-1 is a sym-triazine with diverse biological activities.{53142} It inhibits in vitro amyloid-β (1-42) (Aβ42; Item No. 20574) fibrilization when used at a concentration of 20 µM. TAE-1 inhibits acetylcholinesterase (AChE; IC50 = 0.465 µM for the human erythrocyte enzyme). It also increases neuronal cellular process length and branching and synaptophysin protein levels in differentiated human SH-SY5Y neuronal cells.
Brand:CaymanSKU:20464 -Available on backorder
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TAE-1 is a sym-triazine with diverse biological activities.{53142} It inhibits in vitro amyloid-β (1-42) (Aβ42; Item No. 20574) fibrilization when used at a concentration of 20 µM. TAE-1 inhibits acetylcholinesterase (AChE; IC50 = 0.465 µM for the human erythrocyte enzyme). It also increases neuronal cellular process length and branching and synaptophysin protein levels in differentiated human SH-SY5Y neuronal cells.
Brand:CaymanSKU:20464 -Available on backorder
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Human anaplastic lymphoma kinase (ALK) is an oncogene that is amplified in neuroblastomas and when juxtaposed with various fusion partners, its constitutive kinase activity is associated with the development of a type of anaplastic large cell lymphoma (ALCL).{29085,29086} TAE684 is an ALK inhibitor that blocks the proliferation of ALCL-derived and ALK-dependent cell lines with IC50 values of 2-5 nM.{29085} When tested against a panel of 35 cells transformed by various tyrosine kinases, TAE684 demonstrated 100- to 1,000-fold selectivity for inhibiting ALK-driven cell proliferation.{29085} TAE684 treatment induces cell cycle arrest and apoptosis in ALK-dependent cell lines and has been used to suppress tumor growth in in vivo models of ALK-positive ALCL and neuroblastoma.{29085,29086} TAE684 is also reported to inhibit the activity of the Parkinson’s disease-linked leucine-rich repeat kinase 2 (IC50s = 7.8 and 6.1 nM for wild-type and G2019S mutant LRRK2, respectively).{29087}
Brand:CaymanSKU:-Available on backorder
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Human anaplastic lymphoma kinase (ALK) is an oncogene that is amplified in neuroblastomas and when juxtaposed with various fusion partners, its constitutive kinase activity is associated with the development of a type of anaplastic large cell lymphoma (ALCL).{29085,29086} TAE684 is an ALK inhibitor that blocks the proliferation of ALCL-derived and ALK-dependent cell lines with IC50 values of 2-5 nM.{29085} When tested against a panel of 35 cells transformed by various tyrosine kinases, TAE684 demonstrated 100- to 1,000-fold selectivity for inhibiting ALK-driven cell proliferation.{29085} TAE684 treatment induces cell cycle arrest and apoptosis in ALK-dependent cell lines and has been used to suppress tumor growth in in vivo models of ALK-positive ALCL and neuroblastoma.{29085,29086} TAE684 is also reported to inhibit the activity of the Parkinson’s disease-linked leucine-rich repeat kinase 2 (IC50s = 7.8 and 6.1 nM for wild-type and G2019S mutant LRRK2, respectively).{29087}
Brand:CaymanSKU:-Available on backorder
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Human anaplastic lymphoma kinase (ALK) is an oncogene that is amplified in neuroblastomas and when juxtaposed with various fusion partners, its constitutive kinase activity is associated with the development of a type of anaplastic large cell lymphoma (ALCL).{29085,29086} TAE684 is an ALK inhibitor that blocks the proliferation of ALCL-derived and ALK-dependent cell lines with IC50 values of 2-5 nM.{29085} When tested against a panel of 35 cells transformed by various tyrosine kinases, TAE684 demonstrated 100- to 1,000-fold selectivity for inhibiting ALK-driven cell proliferation.{29085} TAE684 treatment induces cell cycle arrest and apoptosis in ALK-dependent cell lines and has been used to suppress tumor growth in in vivo models of ALK-positive ALCL and neuroblastoma.{29085,29086} TAE684 is also reported to inhibit the activity of the Parkinson’s disease-linked leucine-rich repeat kinase 2 (IC50s = 7.8 and 6.1 nM for wild-type and G2019S mutant LRRK2, respectively).{29087}
Brand:CaymanSKU:-Available on backorder
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Human anaplastic lymphoma kinase (ALK) is an oncogene that is amplified in neuroblastomas and when juxtaposed with various fusion partners, its constitutive kinase activity is associated with the development of a type of anaplastic large cell lymphoma (ALCL).{29085,29086} TAE684 is an ALK inhibitor that blocks the proliferation of ALCL-derived and ALK-dependent cell lines with IC50 values of 2-5 nM.{29085} When tested against a panel of 35 cells transformed by various tyrosine kinases, TAE684 demonstrated 100- to 1,000-fold selectivity for inhibiting ALK-driven cell proliferation.{29085} TAE684 treatment induces cell cycle arrest and apoptosis in ALK-dependent cell lines and has been used to suppress tumor growth in in vivo models of ALK-positive ALCL and neuroblastoma.{29085,29086} TAE684 is also reported to inhibit the activity of the Parkinson’s disease-linked leucine-rich repeat kinase 2 (IC50s = 7.8 and 6.1 nM for wild-type and G2019S mutant LRRK2, respectively).{29087}
Brand:CaymanSKU:-Available on backorder
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Tafamidis is a kinetic stabilizer of transthyretin (TTR) that prevents amyloidogenesis by wild-type and mutant TTRs.{38438} It binds to TTR with negative cooperativity (Kd1 = 3 nM; Kd2 = 278 nM) to stabilize the TTR dimer-dimer interface and inhibit tetrameric dissociation. Tafamidis stabilizes wild-type and clinically significant V30M and V122I mutant TTR amyloidogenic homotetramers (EC50s = 2.7-3.2 μM) under fibril-promoting, denaturing, and physiological conditions in vitro. It stabilizes TTR heterotetramers containing wild-type and mutant subunits ex vivo in human plasma derived from patients carrying V30M or V1221 mutations when used at a concentration of 7.2 μM. Formulations containing tafamidis have been used for the treatment of familial amyloid polyneuropathy.{38439}
Brand:CaymanSKU:- -
A number of 17-phenyl trinor Prostaglandin F2α (Item No. 16810) derivatives have been approved for the treatment of glaucoma.{8941,8322,8839,9311} Of these, the ones wherein the 13,14-double bond has been hydrogenated retain relatively good potency, but show a significantly reduced incidence of local irritant side effects.{9736} Alternatively, it was recently reported that analogs incorporating a 15-deoxy-15,15-difluoro modification also had a favorable ophthalmic activity profile.{11598} Tafluprost is a 2-series, 16-phenoxy analog of PGF2α with the 15,15-difluoro substitution. Tafluprost free acid is a very potent FP receptor agonist, with a Ki of 0.4 nM.{11598} The ester prodrug forms of tafluprost are also potent ocular hypotensives in monkeys.
Brand:CaymanSKU:10005440 - 1 mgAvailable on backorder
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A number of 17-phenyl trinor Prostaglandin F2α (Item No. 16810) derivatives have been approved for the treatment of glaucoma.{8941,8322,8839,9311} Of these, the ones wherein the 13,14-double bond has been hydrogenated retain relatively good potency, but show a significantly reduced incidence of local irritant side effects.{9736} Alternatively, it was recently reported that analogs incorporating a 15-deoxy-15,15-difluoro modification also had a favorable ophthalmic activity profile.{11598} Tafluprost is a 2-series, 16-phenoxy analog of PGF2α with the 15,15-difluoro substitution. Tafluprost free acid is a very potent FP receptor agonist, with a Ki of 0.4 nM.{11598} The ester prodrug forms of tafluprost are also potent ocular hypotensives in monkeys.
Brand:CaymanSKU:10005440 - 10 mgAvailable on backorder
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A number of 17-phenyl trinor Prostaglandin F2α (Item No. 16810) derivatives have been approved for the treatment of glaucoma.{8941,8322,8839,9311} Of these, the ones wherein the 13,14-double bond has been hydrogenated retain relatively good potency, but show a significantly reduced incidence of local irritant side effects.{9736} Alternatively, it was recently reported that analogs incorporating a 15-deoxy-15,15-difluoro modification also had a favorable ophthalmic activity profile.{11598} Tafluprost is a 2-series, 16-phenoxy analog of PGF2α with the 15,15-difluoro substitution. Tafluprost free acid is a very potent FP receptor agonist, with a Ki of 0.4 nM.{11598} The ester prodrug forms of tafluprost are also potent ocular hypotensives in monkeys.
Brand:CaymanSKU:10005440 - 25 mgAvailable on backorder
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A number of 17-phenyl trinor Prostaglandin F2α (Item No. 16810) derivatives have been approved for the treatment of glaucoma.{8941,8322,8839,9311} Of these, the ones wherein the 13,14-double bond has been hydrogenated retain relatively good potency, but show a significantly reduced incidence of local irritant side effects.{9736} Alternatively, it was recently reported that analogs incorporating a 15-deoxy-15,15-difluoro modification also had a favorable ophthalmic activity profile.{11598} Tafluprost is a 2-series, 16-phenoxy analog of PGF2α with the 15,15-difluoro substitution. Tafluprost free acid is a very potent FP receptor agonist, with a Ki of 0.4 nM.{11598} The ester prodrug forms of tafluprost are also potent ocular hypotensives in monkeys.
Brand:CaymanSKU:10005440 - 5 mgAvailable on backorder
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A number of 17-phenyl trinor prostaglandin F2α (17-phenyl trinor PGF2α) derivatives have been approved for the treatment of glaucoma.{8941,8322,8839,9311} Of these, the ones wherein the 13,14-double bond has been hydrogenated retain relatively good potency, but show a significantly reduced incidence of local irritant side effects.{9736} Alternatively, it was recently reported that analogs incorporating a 15-deoxy-15,15-difluoro modification also had a favorable ophthalmic activity profile.{12141} Tafluprost is a 2-series, 16-phenoxy analog of PGF2α with the 15,15-difluoro substitution. Tafluprost (free acid) is a very potent FP receptor agonist, with a Ki of 0.4 nM.{12141} The ester prodrug forms of tafluprost are also potent ocular hypotensives in monkeys.
Brand:CaymanSKU:10005439 - 1 mgAvailable on backorder
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A number of 17-phenyl trinor prostaglandin F2α (17-phenyl trinor PGF2α) derivatives have been approved for the treatment of glaucoma.{8941,8322,8839,9311} Of these, the ones wherein the 13,14-double bond has been hydrogenated retain relatively good potency, but show a significantly reduced incidence of local irritant side effects.{9736} Alternatively, it was recently reported that analogs incorporating a 15-deoxy-15,15-difluoro modification also had a favorable ophthalmic activity profile.{12141} Tafluprost is a 2-series, 16-phenoxy analog of PGF2α with the 15,15-difluoro substitution. Tafluprost (free acid) is a very potent FP receptor agonist, with a Ki of 0.4 nM.{12141} The ester prodrug forms of tafluprost are also potent ocular hypotensives in monkeys.
Brand:CaymanSKU:10005439 - 10 mgAvailable on backorder
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A number of 17-phenyl trinor prostaglandin F2α (17-phenyl trinor PGF2α) derivatives have been approved for the treatment of glaucoma.{8941,8322,8839,9311} Of these, the ones wherein the 13,14-double bond has been hydrogenated retain relatively good potency, but show a significantly reduced incidence of local irritant side effects.{9736} Alternatively, it was recently reported that analogs incorporating a 15-deoxy-15,15-difluoro modification also had a favorable ophthalmic activity profile.{12141} Tafluprost is a 2-series, 16-phenoxy analog of PGF2α with the 15,15-difluoro substitution. Tafluprost (free acid) is a very potent FP receptor agonist, with a Ki of 0.4 nM.{12141} The ester prodrug forms of tafluprost are also potent ocular hypotensives in monkeys.
Brand:CaymanSKU:10005439 - 25 mgAvailable on backorder
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A number of 17-phenyl trinor prostaglandin F2α (17-phenyl trinor PGF2α) derivatives have been approved for the treatment of glaucoma.{8941,8322,8839,9311} Of these, the ones wherein the 13,14-double bond has been hydrogenated retain relatively good potency, but show a significantly reduced incidence of local irritant side effects.{9736} Alternatively, it was recently reported that analogs incorporating a 15-deoxy-15,15-difluoro modification also had a favorable ophthalmic activity profile.{12141} Tafluprost is a 2-series, 16-phenoxy analog of PGF2α with the 15,15-difluoro substitution. Tafluprost (free acid) is a very potent FP receptor agonist, with a Ki of 0.4 nM.{12141} The ester prodrug forms of tafluprost are also potent ocular hypotensives in monkeys.
Brand:CaymanSKU:10005439 - 5 mgAvailable on backorder
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Tafluprost ethyl amide is derived from 17-phenyl trinor Prostaglandin F2α(17-phenyl trinor PGF2α). A number of 17-phenyl trinor PGF2α derivatives have been approved for the treatment of glaucoma.{8941,8322,8839,9311} Of these, the ones wherein the 13,14-double bond has been hydrogenated retain relatively good potency, but show a significantly reduced incidence of local irritant side effects.{9736} Alternatively, it was recently reported that analogs incorporating a 15-deoxy-15,15-difluoro modification also had a favorable ophthalmic activity profile.{11598} Tafluprost is a 2-series, 16-phenoxy analog of PGF2α with the 15,15-difluoro substitution. As a free acid, Tafluprost is a very potent FP receptor agonist (Ki = 0.4 nM).{11598} Ethyl amides of PGs tend to increase lipid solubility, to improve uptake into tissues and to further lower the effective concentration.
Brand:CaymanSKU:9000843 - 1 mgAvailable on backorder
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Tafluprost ethyl amide is derived from 17-phenyl trinor Prostaglandin F2α(17-phenyl trinor PGF2α). A number of 17-phenyl trinor PGF2α derivatives have been approved for the treatment of glaucoma.{8941,8322,8839,9311} Of these, the ones wherein the 13,14-double bond has been hydrogenated retain relatively good potency, but show a significantly reduced incidence of local irritant side effects.{9736} Alternatively, it was recently reported that analogs incorporating a 15-deoxy-15,15-difluoro modification also had a favorable ophthalmic activity profile.{11598} Tafluprost is a 2-series, 16-phenoxy analog of PGF2α with the 15,15-difluoro substitution. As a free acid, Tafluprost is a very potent FP receptor agonist (Ki = 0.4 nM).{11598} Ethyl amides of PGs tend to increase lipid solubility, to improve uptake into tissues and to further lower the effective concentration.
Brand:CaymanSKU:9000843 - 10 mgAvailable on backorder
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Tafluprost ethyl amide is derived from 17-phenyl trinor Prostaglandin F2α(17-phenyl trinor PGF2α). A number of 17-phenyl trinor PGF2α derivatives have been approved for the treatment of glaucoma.{8941,8322,8839,9311} Of these, the ones wherein the 13,14-double bond has been hydrogenated retain relatively good potency, but show a significantly reduced incidence of local irritant side effects.{9736} Alternatively, it was recently reported that analogs incorporating a 15-deoxy-15,15-difluoro modification also had a favorable ophthalmic activity profile.{11598} Tafluprost is a 2-series, 16-phenoxy analog of PGF2α with the 15,15-difluoro substitution. As a free acid, Tafluprost is a very potent FP receptor agonist (Ki = 0.4 nM).{11598} Ethyl amides of PGs tend to increase lipid solubility, to improve uptake into tissues and to further lower the effective concentration.
Brand:CaymanSKU:9000843 - 25 mgAvailable on backorder
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Tafluprost ethyl amide is derived from 17-phenyl trinor Prostaglandin F2α(17-phenyl trinor PGF2α). A number of 17-phenyl trinor PGF2α derivatives have been approved for the treatment of glaucoma.{8941,8322,8839,9311} Of these, the ones wherein the 13,14-double bond has been hydrogenated retain relatively good potency, but show a significantly reduced incidence of local irritant side effects.{9736} Alternatively, it was recently reported that analogs incorporating a 15-deoxy-15,15-difluoro modification also had a favorable ophthalmic activity profile.{11598} Tafluprost is a 2-series, 16-phenoxy analog of PGF2α with the 15,15-difluoro substitution. As a free acid, Tafluprost is a very potent FP receptor agonist (Ki = 0.4 nM).{11598} Ethyl amides of PGs tend to increase lipid solubility, to improve uptake into tissues and to further lower the effective concentration.
Brand:CaymanSKU:9000843 - 5 mgAvailable on backorder
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Analogs of prostaglandin F2α (PGF2α), which act primarily at the FP receptor, have been approved for the treatment of glaucoma.{16991,13707,20816,20817} Tafluprost (free acid) (Item No. 10005439) is a PGF2α analog which acts as a potent FP receptor agonist (Ki = 0.4 nM).{12141} Tafluprost ethyl ester is a form of tafluprost which may have increased lipid solubility compared to the free acid. In addition, the ethyl ester form may demonstrate improved uptake into tissues and thus lower the effective concentration.
Brand:CaymanSKU:11612 - 1 mgAvailable on backorder
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Analogs of prostaglandin F2α (PGF2α), which act primarily at the FP receptor, have been approved for the treatment of glaucoma.{16991,13707,20816,20817} Tafluprost (free acid) (Item No. 10005439) is a PGF2α analog which acts as a potent FP receptor agonist (Ki = 0.4 nM).{12141} Tafluprost ethyl ester is a form of tafluprost which may have increased lipid solubility compared to the free acid. In addition, the ethyl ester form may demonstrate improved uptake into tissues and thus lower the effective concentration.
Brand:CaymanSKU:11612 - 10 mgAvailable on backorder
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Analogs of prostaglandin F2α (PGF2α), which act primarily at the FP receptor, have been approved for the treatment of glaucoma.{16991,13707,20816,20817} Tafluprost (free acid) (Item No. 10005439) is a PGF2α analog which acts as a potent FP receptor agonist (Ki = 0.4 nM).{12141} Tafluprost ethyl ester is a form of tafluprost which may have increased lipid solubility compared to the free acid. In addition, the ethyl ester form may demonstrate improved uptake into tissues and thus lower the effective concentration.
Brand:CaymanSKU:11612 - 5 mgAvailable on backorder
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TAK-063 is a potent inhibitor of phosphodiesterase 10A (PDE10A; IC50 = 0.3 nM).{38458} It is >15,000-fold selective for PDE10A over other PDEs and exhibits 14276 | ISO60194) with a minimum effective dose (MED) of 0.3 mg/kg, p.o., in wild-type mice but has no effect in PDE10A knockout mice at doses up to 1 mg/kg. TAK-063 also reverses hyperlocomotion induced by (+)-MK-801 (Item No. 10009019) (MED = 0.1 mg/kg, p.o.) but has no effect on plasma prolactin or glucose levels in rats.{38459}
Brand:CaymanSKU:22208 -Out of stock
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TAK-063 is a potent inhibitor of phosphodiesterase 10A (PDE10A; IC50 = 0.3 nM).{38458} It is >15,000-fold selective for PDE10A over other PDEs and exhibits 14276 | ISO60194) with a minimum effective dose (MED) of 0.3 mg/kg, p.o., in wild-type mice but has no effect in PDE10A knockout mice at doses up to 1 mg/kg. TAK-063 also reverses hyperlocomotion induced by (+)-MK-801 (Item No. 10009019) (MED = 0.1 mg/kg, p.o.) but has no effect on plasma prolactin or glucose levels in rats.{38459}
Brand:CaymanSKU:22208 -Out of stock
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TAK-063 is a potent inhibitor of phosphodiesterase 10A (PDE10A; IC50 = 0.3 nM).{38458} It is >15,000-fold selective for PDE10A over other PDEs and exhibits 14276 | ISO60194) with a minimum effective dose (MED) of 0.3 mg/kg, p.o., in wild-type mice but has no effect in PDE10A knockout mice at doses up to 1 mg/kg. TAK-063 also reverses hyperlocomotion induced by (+)-MK-801 (Item No. 10009019) (MED = 0.1 mg/kg, p.o.) but has no effect on plasma prolactin or glucose levels in rats.{38459}
Brand:CaymanSKU:22208 -Out of stock
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TAK-063 is a potent inhibitor of phosphodiesterase 10A (PDE10A; IC50 = 0.3 nM).{38458} It is >15,000-fold selective for PDE10A over other PDEs and exhibits 14276 | ISO60194) with a minimum effective dose (MED) of 0.3 mg/kg, p.o., in wild-type mice but has no effect in PDE10A knockout mice at doses up to 1 mg/kg. TAK-063 also reverses hyperlocomotion induced by (+)-MK-801 (Item No. 10009019) (MED = 0.1 mg/kg, p.o.) but has no effect on plasma prolactin or glucose levels in rats.{38459}
Brand:CaymanSKU:22208 -Out of stock
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TAK-220 is an orally bioavailable antagonist of chemokine (C-C motif) receptor 5 (CCR5).{46460} It binds to CCR5 (IC50 = 3.5 nM for the human receptor in CHO cells), but not CCR1, CCR2b, CCR3, CCR4, or CCR7.{46460,46459} TAK-220 inhibits the binding of chemokine (C-C motif) ligand 5 (CCL5) and CCL3 to CCR5 (IC50s = 3.5 and 1.4 nM, respectively) but does not inhibit binding of CCL4.{46459} It inhibits HIV-1 envelope-mediated membrane fusion in a macrophage (M-tropic) R5, but not in a T cell (T-tropic) X4, strain of HIV-1 (IC50s = 0.42 and >1,000 nM, respectively). TAK-220 inhibits the replication of six strains of R5 HIV-1 clinical isolates (EC90 overall mean = 13 nM) and the R5 JR-FL laboratory-adapted strain (EC50 = 0.6 nM), but not of X4 HIV-1 clinical isolates or the X4 IIIB laboratory-adapted strain (EC50s = >10,000 nM for both), in human peripheral blood mononuclear cells (PBMCs).
Brand:CaymanSKU:28448 - 1 mgAvailable on backorder
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Toll-like receptor 4 (TLR4) is activated by lipopolysaccharide (LPS), with LPS-binding protein, to initiate an innate immune response.{28195} Alternatively, hypoxia or ischemia/reperfusion can trigger signaling through TLR4.{28194} TAK-242 is a cell-permeable inhibitor of TLR4 signaling, blocking LPS-induced production of NO, TNF-α, IL-6, and IL-1β in macrophages with IC50 values of 1-11 nM.{28192,28174} It does not affect signaling through other TLRs.{28192,28174,28193} TAK-242 is effective in vivo, suppressing the production of NO, TNF-α, IL-6, and IL-1β in mice treated with LPS when given intravenously.{28192} Mechanistically, TAK-242 acts by selectively binding TLR4 and preventing its association with adaptor proteins that are essential for signal transduction.{28193} TAK-242 is used to study signaling through TLR4 in a variety of pathologies, including sepsis and ischemia/reperfusion injury.{28191,28173}
Brand:CaymanSKU:- -
Toll-like receptor 4 (TLR4) is activated by lipopolysaccharide (LPS), with LPS-binding protein, to initiate an innate immune response.{28195} Alternatively, hypoxia or ischemia/reperfusion can trigger signaling through TLR4.{28194} TAK-242 is a cell-permeable inhibitor of TLR4 signaling, blocking LPS-induced production of NO, TNF-α, IL-6, and IL-1β in macrophages with IC50 values of 1-11 nM.{28192,28174} It does not affect signaling through other TLRs.{28192,28174,28193} TAK-242 is effective in vivo, suppressing the production of NO, TNF-α, IL-6, and IL-1β in mice treated with LPS when given intravenously.{28192} Mechanistically, TAK-242 acts by selectively binding TLR4 and preventing its association with adaptor proteins that are essential for signal transduction.{28193} TAK-242 is used to study signaling through TLR4 in a variety of pathologies, including sepsis and ischemia/reperfusion injury.{28191,28173}
Brand:CaymanSKU:- -
Toll-like receptor 4 (TLR4) is activated by lipopolysaccharide (LPS), with LPS-binding protein, to initiate an innate immune response.{28195} Alternatively, hypoxia or ischemia/reperfusion can trigger signaling through TLR4.{28194} TAK-242 is a cell-permeable inhibitor of TLR4 signaling, blocking LPS-induced production of NO, TNF-α, IL-6, and IL-1β in macrophages with IC50 values of 1-11 nM.{28192,28174} It does not affect signaling through other TLRs.{28192,28174,28193} TAK-242 is effective in vivo, suppressing the production of NO, TNF-α, IL-6, and IL-1β in mice treated with LPS when given intravenously.{28192} Mechanistically, TAK-242 acts by selectively binding TLR4 and preventing its association with adaptor proteins that are essential for signal transduction.{28193} TAK-242 is used to study signaling through TLR4 in a variety of pathologies, including sepsis and ischemia/reperfusion injury.{28191,28173}
Brand:CaymanSKU:- -
Toll-like receptor 4 (TLR4) is activated by lipopolysaccharide (LPS), with LPS-binding protein, to initiate an innate immune response.{28195} Alternatively, hypoxia or ischemia/reperfusion can trigger signaling through TLR4.{28194} TAK-242 is a cell-permeable inhibitor of TLR4 signaling, blocking LPS-induced production of NO, TNF-α, IL-6, and IL-1β in macrophages with IC50 values of 1-11 nM.{28192,28174} It does not affect signaling through other TLRs.{28192,28174,28193} TAK-242 is effective in vivo, suppressing the production of NO, TNF-α, IL-6, and IL-1β in mice treated with LPS when given intravenously.{28192} Mechanistically, TAK-242 acts by selectively binding TLR4 and preventing its association with adaptor proteins that are essential for signal transduction.{28193} TAK-242 is used to study signaling through TLR4 in a variety of pathologies, including sepsis and ischemia/reperfusion injury.{28191,28173}
Brand:CaymanSKU:- -
TAK-385 is an orally bioavailable gonadotropin-releasing hormone receptor (GnRHR) antagonist (IC50s = 0.33 and 0.32 nM for the human and monkey receptors, respectively).{49487} It is selective for these receptors over the rat GnRHR receptor (IC50 = 9,800 nM), as well as a panel of 134 enzymes and receptors at 10 µM. TAK-385 is 95-fold more potent at inhibiting GnRH-induced arachidonic acid (Item Nos. 90010 | 90010.1 | 10006607) release in CHO cells expressing human GnRHR compared with those expressing monkey GnRHR. It decreases testis, ventral prostate, ovary, and uterus weight in human GNRHR knock-in mice when administered at doses ranging from 3 to 200 mg/kg per day for 28 days.{49488} TAK-385 (1 and 3 mg/kg) also decreases plasma luteinizing hormone levels in castrated cynomolgus monkeys.{49487}
Brand:CaymanSKU:29512 - 1 mgAvailable on backorder
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TAK-385 is an orally bioavailable gonadotropin-releasing hormone receptor (GnRHR) antagonist (IC50s = 0.33 and 0.32 nM for the human and monkey receptors, respectively).{49487} It is selective for these receptors over the rat GnRHR receptor (IC50 = 9,800 nM), as well as a panel of 134 enzymes and receptors at 10 µM. TAK-385 is 95-fold more potent at inhibiting GnRH-induced arachidonic acid (Item Nos. 90010 | 90010.1 | 10006607) release in CHO cells expressing human GnRHR compared with those expressing monkey GnRHR. It decreases testis, ventral prostate, ovary, and uterus weight in human GNRHR knock-in mice when administered at doses ranging from 3 to 200 mg/kg per day for 28 days.{49488} TAK-385 (1 and 3 mg/kg) also decreases plasma luteinizing hormone levels in castrated cynomolgus monkeys.{49487}
Brand:CaymanSKU:29512 - 10 mgAvailable on backorder
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TAK-385 is an orally bioavailable gonadotropin-releasing hormone receptor (GnRHR) antagonist (IC50s = 0.33 and 0.32 nM for the human and monkey receptors, respectively).{49487} It is selective for these receptors over the rat GnRHR receptor (IC50 = 9,800 nM), as well as a panel of 134 enzymes and receptors at 10 µM. TAK-385 is 95-fold more potent at inhibiting GnRH-induced arachidonic acid (Item Nos. 90010 | 90010.1 | 10006607) release in CHO cells expressing human GnRHR compared with those expressing monkey GnRHR. It decreases testis, ventral prostate, ovary, and uterus weight in human GNRHR knock-in mice when administered at doses ranging from 3 to 200 mg/kg per day for 28 days.{49488} TAK-385 (1 and 3 mg/kg) also decreases plasma luteinizing hormone levels in castrated cynomolgus monkeys.{49487}
Brand:CaymanSKU:29512 - 25 mgAvailable on backorder
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TAK-385 is an orally bioavailable gonadotropin-releasing hormone receptor (GnRHR) antagonist (IC50s = 0.33 and 0.32 nM for the human and monkey receptors, respectively).{49487} It is selective for these receptors over the rat GnRHR receptor (IC50 = 9,800 nM), as well as a panel of 134 enzymes and receptors at 10 µM. TAK-385 is 95-fold more potent at inhibiting GnRH-induced arachidonic acid (Item Nos. 90010 | 90010.1 | 10006607) release in CHO cells expressing human GnRHR compared with those expressing monkey GnRHR. It decreases testis, ventral prostate, ovary, and uterus weight in human GNRHR knock-in mice when administered at doses ranging from 3 to 200 mg/kg per day for 28 days.{49488} TAK-385 (1 and 3 mg/kg) also decreases plasma luteinizing hormone levels in castrated cynomolgus monkeys.{49487}
Brand:CaymanSKU:29512 - 5 mgAvailable on backorder
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TAK-599 is a prodrug of T-91825, a cephalosporin antibiotic.{37238} In vitro, TAK-599 inhibits growth of S. pneumoniae, S. aureus, methicillin-resistant S. aureus (MRSA), E. coli, and K. pneumoniae (MICs = 0.008-2 mg/L).{37240} It is rapidly converted to T-91825 in rats and monkeys.{37238} TAK-599 has bacteriostatic effects in mice infected with S. pneumoniae, S. aureus, MRSA, E. coli, or K. pneumoniae when administered at doses ranging from 0.2-234 mg/kg per day and also decreases the number of CFUs in a mouse model of thigh infection.{37240} It exhibits a protective effect against systemic infection by clinical MRSA isolates in mice (ED50s = 1.08-4.81 mg/kg).{37239}
Brand:CaymanSKU:23696 - 1 mgAvailable on backorder
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TAK-599 is a prodrug of T-91825, a cephalosporin antibiotic.{37238} In vitro, TAK-599 inhibits growth of S. pneumoniae, S. aureus, methicillin-resistant S. aureus (MRSA), E. coli, and K. pneumoniae (MICs = 0.008-2 mg/L).{37240} It is rapidly converted to T-91825 in rats and monkeys.{37238} TAK-599 has bacteriostatic effects in mice infected with S. pneumoniae, S. aureus, MRSA, E. coli, or K. pneumoniae when administered at doses ranging from 0.2-234 mg/kg per day and also decreases the number of CFUs in a mouse model of thigh infection.{37240} It exhibits a protective effect against systemic infection by clinical MRSA isolates in mice (ED50s = 1.08-4.81 mg/kg).{37239}
Brand:CaymanSKU:23696 - 10 mgAvailable on backorder
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TAK-599 is a prodrug of T-91825, a cephalosporin antibiotic.{37238} In vitro, TAK-599 inhibits growth of S. pneumoniae, S. aureus, methicillin-resistant S. aureus (MRSA), E. coli, and K. pneumoniae (MICs = 0.008-2 mg/L).{37240} It is rapidly converted to T-91825 in rats and monkeys.{37238} TAK-599 has bacteriostatic effects in mice infected with S. pneumoniae, S. aureus, MRSA, E. coli, or K. pneumoniae when administered at doses ranging from 0.2-234 mg/kg per day and also decreases the number of CFUs in a mouse model of thigh infection.{37240} It exhibits a protective effect against systemic infection by clinical MRSA isolates in mice (ED50s = 1.08-4.81 mg/kg).{37239}
Brand:CaymanSKU:23696 - 5 mgAvailable on backorder
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TAK-632 is a slow off-rate inhibitor of Raf kinases (IC50s = 8.3, 2.4, and 1.4 nM for wild type B-Raf, mutant B-RafV600E, and c-Raf, respectively).{28688} It demonstrates 14-1,200-fold selectivity for Raf over a panel of 26 different kinases.{28688} TAK-632 shows significant antiproliferative activity against mutated B-Raf or mutated N-Ras cancer cell lines and xenograft models, inhibiting MEK phosphorylation with an IC50 value of 12 nM and downstream ERK phosphorylation with an IC50 value of 16 nM.{28688,28689}
Brand:CaymanSKU:- -
TAK-632 is a slow off-rate inhibitor of Raf kinases (IC50s = 8.3, 2.4, and 1.4 nM for wild type B-Raf, mutant B-RafV600E, and c-Raf, respectively).{28688} It demonstrates 14-1,200-fold selectivity for Raf over a panel of 26 different kinases.{28688} TAK-632 shows significant antiproliferative activity against mutated B-Raf or mutated N-Ras cancer cell lines and xenograft models, inhibiting MEK phosphorylation with an IC50 value of 12 nM and downstream ERK phosphorylation with an IC50 value of 16 nM.{28688,28689}
Brand:CaymanSKU:- -
TAK-632 is a slow off-rate inhibitor of Raf kinases (IC50s = 8.3, 2.4, and 1.4 nM for wild type B-Raf, mutant B-RafV600E, and c-Raf, respectively).{28688} It demonstrates 14-1,200-fold selectivity for Raf over a panel of 26 different kinases.{28688} TAK-632 shows significant antiproliferative activity against mutated B-Raf or mutated N-Ras cancer cell lines and xenograft models, inhibiting MEK phosphorylation with an IC50 value of 12 nM and downstream ERK phosphorylation with an IC50 value of 16 nM.{28688,28689}
Brand:CaymanSKU:- -
TAK-632 is a slow off-rate inhibitor of Raf kinases (IC50s = 8.3, 2.4, and 1.4 nM for wild type B-Raf, mutant B-RafV600E, and c-Raf, respectively).{28688} It demonstrates 14-1,200-fold selectivity for Raf over a panel of 26 different kinases.{28688} TAK-632 shows significant antiproliferative activity against mutated B-Raf or mutated N-Ras cancer cell lines and xenograft models, inhibiting MEK phosphorylation with an IC50 value of 12 nM and downstream ERK phosphorylation with an IC50 value of 16 nM.{28688,28689}
Brand:CaymanSKU:- -
TAK-715 is an inhibitor of p38α MAPK (IC50 = 7.1 nM).{45144} It is selective for p38α over p38β (IC50 = 200 nM), as well as over p38γ/δ, JNK, ERK1, IKKβ, MEKK1, and TAK1 (IC50 = >10 µM for all) but also inhibits casein kinase Iδ (CK1δ) and CK1ε.{45144,27226} It inhibits TNF-α release induced by LPS from THP-1 cells (IC50 = 48 nM) and inhibits LPS-induced TNF-α production by 87.6% in mice when administered at a dose of 10 mg/kg.{45144} TAK-715 (30 mg/kg) reduces adjuvant-induced paw swelling in a rat model of rheumatoid arthritis. It also inhibits phosphorylation of human Disheveled 2 (hDvl2) by Wnt3a in a p38α-independent manner.{27226}
Brand:CaymanSKU:26170 - 10 mgAvailable on backorder
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TAK-715 is an inhibitor of p38α MAPK (IC50 = 7.1 nM).{45144} It is selective for p38α over p38β (IC50 = 200 nM), as well as over p38γ/δ, JNK, ERK1, IKKβ, MEKK1, and TAK1 (IC50 = >10 µM for all) but also inhibits casein kinase Iδ (CK1δ) and CK1ε.{45144,27226} It inhibits TNF-α release induced by LPS from THP-1 cells (IC50 = 48 nM) and inhibits LPS-induced TNF-α production by 87.6% in mice when administered at a dose of 10 mg/kg.{45144} TAK-715 (30 mg/kg) reduces adjuvant-induced paw swelling in a rat model of rheumatoid arthritis. It also inhibits phosphorylation of human Disheveled 2 (hDvl2) by Wnt3a in a p38α-independent manner.{27226}
Brand:CaymanSKU:26170 - 25 mgAvailable on backorder
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TAK-715 is an inhibitor of p38α MAPK (IC50 = 7.1 nM).{45144} It is selective for p38α over p38β (IC50 = 200 nM), as well as over p38γ/δ, JNK, ERK1, IKKβ, MEKK1, and TAK1 (IC50 = >10 µM for all) but also inhibits casein kinase Iδ (CK1δ) and CK1ε.{45144,27226} It inhibits TNF-α release induced by LPS from THP-1 cells (IC50 = 48 nM) and inhibits LPS-induced TNF-α production by 87.6% in mice when administered at a dose of 10 mg/kg.{45144} TAK-715 (30 mg/kg) reduces adjuvant-induced paw swelling in a rat model of rheumatoid arthritis. It also inhibits phosphorylation of human Disheveled 2 (hDvl2) by Wnt3a in a p38α-independent manner.{27226}
Brand:CaymanSKU:26170 - 5 mgAvailable on backorder
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TAK-715 is an inhibitor of p38α MAPK (IC50 = 7.1 nM).{45144} It is selective for p38α over p38β (IC50 = 200 nM), as well as over p38γ/δ, JNK, ERK1, IKKβ, MEKK1, and TAK1 (IC50 = >10 µM for all) but also inhibits casein kinase Iδ (CK1δ) and CK1ε.{45144,27226} It inhibits TNF-α release induced by LPS from THP-1 cells (IC50 = 48 nM) and inhibits LPS-induced TNF-α production by 87.6% in mice when administered at a dose of 10 mg/kg.{45144} TAK-715 (30 mg/kg) reduces adjuvant-induced paw swelling in a rat model of rheumatoid arthritis. It also inhibits phosphorylation of human Disheveled 2 (hDvl2) by Wnt3a in a p38α-independent manner.{27226}
Brand:CaymanSKU:26170 - 50 mgAvailable on backorder
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TAK-733 is an inhibitor of MEK1 (IC50 = 3.2 nM), a MAP kinase in the Raf/MEK/ERK pathway that plays a major role in the regulation of cellular growth, differentiation, and proliferation.{37319},{17156} It is selective for MEK1 over a panel of 18 kinases, receptors, and ion channels up to a concentration of 10 µM. TAK-733 inhibits ERK phosphorylation in vitro (EC50 = 1.9 nM). It also inhibits proliferation of A375 and COLO 205 cells (EC50s = 3.1 and 2.1 nM, respectively) and 14 cutaneous melanoma cell lines (IC50s = V600E mutations.{37319},{37320} TAK-733 has antitumor activity in mouse xenograft models using a variety of cancer types.{37319}
Brand:CaymanSKU:-Out of stock
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TAK-733 is an inhibitor of MEK1 (IC50 = 3.2 nM), a MAP kinase in the Raf/MEK/ERK pathway that plays a major role in the regulation of cellular growth, differentiation, and proliferation.{37319},{17156} It is selective for MEK1 over a panel of 18 kinases, receptors, and ion channels up to a concentration of 10 µM. TAK-733 inhibits ERK phosphorylation in vitro (EC50 = 1.9 nM). It also inhibits proliferation of A375 and COLO 205 cells (EC50s = 3.1 and 2.1 nM, respectively) and 14 cutaneous melanoma cell lines (IC50s = V600E mutations.{37319},{37320} TAK-733 has antitumor activity in mouse xenograft models using a variety of cancer types.{37319}
Brand:CaymanSKU:-Out of stock
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TAK-733 is an inhibitor of MEK1 (IC50 = 3.2 nM), a MAP kinase in the Raf/MEK/ERK pathway that plays a major role in the regulation of cellular growth, differentiation, and proliferation.{37319},{17156} It is selective for MEK1 over a panel of 18 kinases, receptors, and ion channels up to a concentration of 10 µM. TAK-733 inhibits ERK phosphorylation in vitro (EC50 = 1.9 nM). It also inhibits proliferation of A375 and COLO 205 cells (EC50s = 3.1 and 2.1 nM, respectively) and 14 cutaneous melanoma cell lines (IC50s = V600E mutations.{37319},{37320} TAK-733 has antitumor activity in mouse xenograft models using a variety of cancer types.{37319}
Brand:CaymanSKU:-Out of stock
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TAK-733 is an inhibitor of MEK1 (IC50 = 3.2 nM), a MAP kinase in the Raf/MEK/ERK pathway that plays a major role in the regulation of cellular growth, differentiation, and proliferation.{37319},{17156} It is selective for MEK1 over a panel of 18 kinases, receptors, and ion channels up to a concentration of 10 µM. TAK-733 inhibits ERK phosphorylation in vitro (EC50 = 1.9 nM). It also inhibits proliferation of A375 and COLO 205 cells (EC50s = 3.1 and 2.1 nM, respectively) and 14 cutaneous melanoma cell lines (IC50s = V600E mutations.{37319},{37320} TAK-733 has antitumor activity in mouse xenograft models using a variety of cancer types.{37319}
Brand:CaymanSKU:-Out of stock
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TAK-779 is an antagonist of chemokine receptor 5 (CCR5), CCR2b, and CXC chemokine receptor 3 (CXCR3).{48138,48139} It inhibits CCR5 and CXCR3 (IC50s = 236 and 369 nM, respectively, for mouse recombinant receptors expressed in 2B4 T cells) and CCR5 and CCR2b (IC50s = 1.4 and 27 nM, respectively, for human recombinant receptors expressed in CHO cells). TAK-779 inhibits the replication of clinical isolates of R5, but not X4, HIV-1 in human peripheral blood mononuclear cells (PBMCs; EC50s = 1.6-3.5 and >20,000 nM, respectively).{48138} TAK-779 (250 mg/animal per day) inhibits ovalbumin-induced increases in CCR5, CXCR3, IFN-γ, and TNF-α expression in mouse lung, as well as the number of total cells, lymphocytes, and eosinophils in bronchoalveolar lavage fluid (BALF), in a mouse model of asthma.{48140} It also increases intestinal allograft survival in a rat model of small intestine transplantation when administered at a dose of 10 mg/kg per day.{48141}
Brand:CaymanSKU:26744 - 1 mgAvailable on backorder
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TAK-779 is an antagonist of chemokine receptor 5 (CCR5), CCR2b, and CXC chemokine receptor 3 (CXCR3).{48138,48139} It inhibits CCR5 and CXCR3 (IC50s = 236 and 369 nM, respectively, for mouse recombinant receptors expressed in 2B4 T cells) and CCR5 and CCR2b (IC50s = 1.4 and 27 nM, respectively, for human recombinant receptors expressed in CHO cells). TAK-779 inhibits the replication of clinical isolates of R5, but not X4, HIV-1 in human peripheral blood mononuclear cells (PBMCs; EC50s = 1.6-3.5 and >20,000 nM, respectively).{48138} TAK-779 (250 mg/animal per day) inhibits ovalbumin-induced increases in CCR5, CXCR3, IFN-γ, and TNF-α expression in mouse lung, as well as the number of total cells, lymphocytes, and eosinophils in bronchoalveolar lavage fluid (BALF), in a mouse model of asthma.{48140} It also increases intestinal allograft survival in a rat model of small intestine transplantation when administered at a dose of 10 mg/kg per day.{48141}
Brand:CaymanSKU:26744 - 10 mgAvailable on backorder
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TAK-779 is an antagonist of chemokine receptor 5 (CCR5), CCR2b, and CXC chemokine receptor 3 (CXCR3).{48138,48139} It inhibits CCR5 and CXCR3 (IC50s = 236 and 369 nM, respectively, for mouse recombinant receptors expressed in 2B4 T cells) and CCR5 and CCR2b (IC50s = 1.4 and 27 nM, respectively, for human recombinant receptors expressed in CHO cells). TAK-779 inhibits the replication of clinical isolates of R5, but not X4, HIV-1 in human peripheral blood mononuclear cells (PBMCs; EC50s = 1.6-3.5 and >20,000 nM, respectively).{48138} TAK-779 (250 mg/animal per day) inhibits ovalbumin-induced increases in CCR5, CXCR3, IFN-γ, and TNF-α expression in mouse lung, as well as the number of total cells, lymphocytes, and eosinophils in bronchoalveolar lavage fluid (BALF), in a mouse model of asthma.{48140} It also increases intestinal allograft survival in a rat model of small intestine transplantation when administered at a dose of 10 mg/kg per day.{48141}
Brand:CaymanSKU:26744 - 25 mgAvailable on backorder
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TAK-779 is an antagonist of chemokine receptor 5 (CCR5), CCR2b, and CXC chemokine receptor 3 (CXCR3).{48138,48139} It inhibits CCR5 and CXCR3 (IC50s = 236 and 369 nM, respectively, for mouse recombinant receptors expressed in 2B4 T cells) and CCR5 and CCR2b (IC50s = 1.4 and 27 nM, respectively, for human recombinant receptors expressed in CHO cells). TAK-779 inhibits the replication of clinical isolates of R5, but not X4, HIV-1 in human peripheral blood mononuclear cells (PBMCs; EC50s = 1.6-3.5 and >20,000 nM, respectively).{48138} TAK-779 (250 mg/animal per day) inhibits ovalbumin-induced increases in CCR5, CXCR3, IFN-γ, and TNF-α expression in mouse lung, as well as the number of total cells, lymphocytes, and eosinophils in bronchoalveolar lavage fluid (BALF), in a mouse model of asthma.{48140} It also increases intestinal allograft survival in a rat model of small intestine transplantation when administered at a dose of 10 mg/kg per day.{48141}
Brand:CaymanSKU:26744 - 5 mgAvailable on backorder
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The free fatty acid receptor 1 (FFAR1; GPR40) is highly expressed in pancreatic β-cells and activated by medium and long-chain fatty acids.{13138} There is evidence of a link between FFAR1 (GPR40) and the ability of fatty acids to amplify glucose-stimulated insulin secretion, making this signaling pathway a potential target for regulating diabetes, obesity, and other metabolic disorders.{13139,14742} TAK-875 is a selective FFAR1 (GPR40) agonist (EC50 = 26 nM) that does not exhibit activity on the related FFARs FFAR2 (GPR43) or FFAR3 (GPR41).{21349}
Brand:CaymanSKU:-Available on backorder
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The free fatty acid receptor 1 (FFAR1; GPR40) is highly expressed in pancreatic β-cells and activated by medium and long-chain fatty acids.{13138} There is evidence of a link between FFAR1 (GPR40) and the ability of fatty acids to amplify glucose-stimulated insulin secretion, making this signaling pathway a potential target for regulating diabetes, obesity, and other metabolic disorders.{13139,14742} TAK-875 is a selective FFAR1 (GPR40) agonist (EC50 = 26 nM) that does not exhibit activity on the related FFARs FFAR2 (GPR43) or FFAR3 (GPR41).{21349}
Brand:CaymanSKU:-Available on backorder
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The free fatty acid receptor 1 (FFAR1; GPR40) is highly expressed in pancreatic β-cells and activated by medium and long-chain fatty acids.{13138} There is evidence of a link between FFAR1 (GPR40) and the ability of fatty acids to amplify glucose-stimulated insulin secretion, making this signaling pathway a potential target for regulating diabetes, obesity, and other metabolic disorders.{13139,14742} TAK-875 is a selective FFAR1 (GPR40) agonist (EC50 = 26 nM) that does not exhibit activity on the related FFARs FFAR2 (GPR43) or FFAR3 (GPR41).{21349}
Brand:CaymanSKU:-Available on backorder
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The free fatty acid receptor 1 (FFAR1; GPR40) is highly expressed in pancreatic β-cells and activated by medium and long-chain fatty acids.{13138} There is evidence of a link between FFAR1 (GPR40) and the ability of fatty acids to amplify glucose-stimulated insulin secretion, making this signaling pathway a potential target for regulating diabetes, obesity, and other metabolic disorders.{13139,14742} TAK-875 is a selective FFAR1 (GPR40) agonist (EC50 = 26 nM) that does not exhibit activity on the related FFARs FFAR2 (GPR43) or FFAR3 (GPR41).{21349}
Brand:CaymanSKU:-Available on backorder
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TAK-901 is a non-selective Aurora kinase inhibitor (IC50s = 3.1, 10, and 4.2 nM for Aurora A, B, and C, respectively).{38687} It also inhibits JAK3, c-Src, CLK2, FGR, YES1, LRRK2, FLT3, Fyn, Abl, and FGFR2 (IC50s = 1.2-6.4 nM) and several other kinases. TAK-901 inhibits Aurora kinase complexes with IC50 values of 21 and 15 nM for the Aurora A and targeting protein for Xklp2 (TPX2) and Aurora B and inner centromere protein (INCENP) complexes, respectively. It decreases histone H3 phosphorylation in human prostate PC3 cancer cells (EC50 = 0.16 μM) and inhibits c-Src, FAK, FGFR2, FLT3, Abl, and Axl autophosphorylation in a panel of cancer cell lines (EC50s = 0.19-3.7 μM). TAK-901 inhibits the growth of lung, colon, stomach, skin, kidney, breast, ovarian, uterine, and prostate cancer cell lines (EC50s = 0.043-1.5 μM). In vivo, TAK-901 (40 mg/kg per day, i.v.) inhibits histone H3 phosphorylation and reduces tumor growth in an A2780 ovarian cancer nude rat xenograft model. TAK-901 also inhibits tumor growth in colorectal, acute myeloid leukemia (AML), and chronic myeloid leukemia (CML) mouse xenograft models.
Brand:CaymanSKU:23772 - 1 mgAvailable on backorder
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TAK-901 is a non-selective Aurora kinase inhibitor (IC50s = 3.1, 10, and 4.2 nM for Aurora A, B, and C, respectively).{38687} It also inhibits JAK3, c-Src, CLK2, FGR, YES1, LRRK2, FLT3, Fyn, Abl, and FGFR2 (IC50s = 1.2-6.4 nM) and several other kinases. TAK-901 inhibits Aurora kinase complexes with IC50 values of 21 and 15 nM for the Aurora A and targeting protein for Xklp2 (TPX2) and Aurora B and inner centromere protein (INCENP) complexes, respectively. It decreases histone H3 phosphorylation in human prostate PC3 cancer cells (EC50 = 0.16 μM) and inhibits c-Src, FAK, FGFR2, FLT3, Abl, and Axl autophosphorylation in a panel of cancer cell lines (EC50s = 0.19-3.7 μM). TAK-901 inhibits the growth of lung, colon, stomach, skin, kidney, breast, ovarian, uterine, and prostate cancer cell lines (EC50s = 0.043-1.5 μM). In vivo, TAK-901 (40 mg/kg per day, i.v.) inhibits histone H3 phosphorylation and reduces tumor growth in an A2780 ovarian cancer nude rat xenograft model. TAK-901 also inhibits tumor growth in colorectal, acute myeloid leukemia (AML), and chronic myeloid leukemia (CML) mouse xenograft models.
Brand:CaymanSKU:23772 - 10 mgAvailable on backorder
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TAK-901 is a non-selective Aurora kinase inhibitor (IC50s = 3.1, 10, and 4.2 nM for Aurora A, B, and C, respectively).{38687} It also inhibits JAK3, c-Src, CLK2, FGR, YES1, LRRK2, FLT3, Fyn, Abl, and FGFR2 (IC50s = 1.2-6.4 nM) and several other kinases. TAK-901 inhibits Aurora kinase complexes with IC50 values of 21 and 15 nM for the Aurora A and targeting protein for Xklp2 (TPX2) and Aurora B and inner centromere protein (INCENP) complexes, respectively. It decreases histone H3 phosphorylation in human prostate PC3 cancer cells (EC50 = 0.16 μM) and inhibits c-Src, FAK, FGFR2, FLT3, Abl, and Axl autophosphorylation in a panel of cancer cell lines (EC50s = 0.19-3.7 μM). TAK-901 inhibits the growth of lung, colon, stomach, skin, kidney, breast, ovarian, uterine, and prostate cancer cell lines (EC50s = 0.043-1.5 μM). In vivo, TAK-901 (40 mg/kg per day, i.v.) inhibits histone H3 phosphorylation and reduces tumor growth in an A2780 ovarian cancer nude rat xenograft model. TAK-901 also inhibits tumor growth in colorectal, acute myeloid leukemia (AML), and chronic myeloid leukemia (CML) mouse xenograft models.
Brand:CaymanSKU:23772 - 25 mgAvailable on backorder
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TAK-901 is a non-selective Aurora kinase inhibitor (IC50s = 3.1, 10, and 4.2 nM for Aurora A, B, and C, respectively).{38687} It also inhibits JAK3, c-Src, CLK2, FGR, YES1, LRRK2, FLT3, Fyn, Abl, and FGFR2 (IC50s = 1.2-6.4 nM) and several other kinases. TAK-901 inhibits Aurora kinase complexes with IC50 values of 21 and 15 nM for the Aurora A and targeting protein for Xklp2 (TPX2) and Aurora B and inner centromere protein (INCENP) complexes, respectively. It decreases histone H3 phosphorylation in human prostate PC3 cancer cells (EC50 = 0.16 μM) and inhibits c-Src, FAK, FGFR2, FLT3, Abl, and Axl autophosphorylation in a panel of cancer cell lines (EC50s = 0.19-3.7 μM). TAK-901 inhibits the growth of lung, colon, stomach, skin, kidney, breast, ovarian, uterine, and prostate cancer cell lines (EC50s = 0.043-1.5 μM). In vivo, TAK-901 (40 mg/kg per day, i.v.) inhibits histone H3 phosphorylation and reduces tumor growth in an A2780 ovarian cancer nude rat xenograft model. TAK-901 also inhibits tumor growth in colorectal, acute myeloid leukemia (AML), and chronic myeloid leukemia (CML) mouse xenograft models.
Brand:CaymanSKU:23772 - 5 mgAvailable on backorder
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Polo-like kinases (Plks) are serine/threonine kinases with key roles in cell cycling. TAK-960 is an orally bioavailable, selective inhibitor of Plks with IC50 values of 0.8, 16.9, and 50.2 nM for Plk1, Plk2, and Plk3, respectively.{31040,31041} It exhibits greater than 20-fold selectivity for Plk1 over FAK, MLCK, and the tyrosine protein kinase Fes, and has minimal activity against a panel of 282 other kinases.{31040,31041} It inhibits the proliferation of various cancer cell lines, including MDR1-expressing tumors, and also prevents tumor growth in several human cancer cell xenograft models, including a disseminated model of AML- and MDR1-expressing hematological tumors.{31040,31041}
Brand:CaymanSKU:-Available on backorder
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Polo-like kinases (Plks) are serine/threonine kinases with key roles in cell cycling. TAK-960 is an orally bioavailable, selective inhibitor of Plks with IC50 values of 0.8, 16.9, and 50.2 nM for Plk1, Plk2, and Plk3, respectively.{31040,31041} It exhibits greater than 20-fold selectivity for Plk1 over FAK, MLCK, and the tyrosine protein kinase Fes, and has minimal activity against a panel of 282 other kinases.{31040,31041} It inhibits the proliferation of various cancer cell lines, including MDR1-expressing tumors, and also prevents tumor growth in several human cancer cell xenograft models, including a disseminated model of AML- and MDR1-expressing hematological tumors.{31040,31041}
Brand:CaymanSKU:-Available on backorder
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Polo-like kinases (Plks) are serine/threonine kinases with key roles in cell cycling. TAK-960 is an orally bioavailable, selective inhibitor of Plks with IC50 values of 0.8, 16.9, and 50.2 nM for Plk1, Plk2, and Plk3, respectively.{31040,31041} It exhibits greater than 20-fold selectivity for Plk1 over FAK, MLCK, and the tyrosine protein kinase Fes, and has minimal activity against a panel of 282 other kinases.{31040,31041} It inhibits the proliferation of various cancer cell lines, including MDR1-expressing tumors, and also prevents tumor growth in several human cancer cell xenograft models, including a disseminated model of AML- and MDR1-expressing hematological tumors.{31040,31041}
Brand:CaymanSKU:-Available on backorder
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Polo-like kinases (Plks) are serine/threonine kinases with key roles in cell cycling. TAK-960 is an orally bioavailable, selective inhibitor of Plks with IC50 values of 0.8, 16.9, and 50.2 nM for Plk1, Plk2, and Plk3, respectively.{31040,31041} It exhibits greater than 20-fold selectivity for Plk1 over FAK, MLCK, and the tyrosine protein kinase Fes, and has minimal activity against a panel of 282 other kinases.{31040,31041} It inhibits the proliferation of various cancer cell lines, including MDR1-expressing tumors, and also prevents tumor growth in several human cancer cell xenograft models, including a disseminated model of AML- and MDR1-expressing hematological tumors.{31040,31041}
Brand:CaymanSKU:-Available on backorder
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Takinib is a TGF-β-activated kinase 1 (TAK1) inhibitor (IC50 = 9.5 nM).{40308} It is selective for TAK1 over IRAK1, IRAK4, GCK, Clk2, and MINK1 (IC50s = 390, 120, 430, 430, and 1,900 nM, respectively). Takinib increases caspase-3/-7 activity and inhibits proliferation of TNF-α-stimulated, but not unstimulated, MDA-MB-231 cells in a concentration-dependent manner. It reduces phosphorylation of IKK, p38 MAPK, MAPK8, MAPK9, and c-Jun in TNF-α-stimulated MDA-MB-231 cells. Takinib inhibits IL-6 secretion in TNF-α-stimulated rheumatoid arthritis fibroblast-like synoviocytes in a concentration-dependent manner. It reduces inflammation and cartilage damage in knee joints in a mouse model of collagen type II-induced arthritis when administered at a dose of 50 mg/kg per day.{57119}
Brand:CaymanSKU:24161 - 1 mgAvailable on backorder
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Takinib is a TGF-β-activated kinase 1 (TAK1) inhibitor (IC50 = 9.5 nM).{40308} It is selective for TAK1 over IRAK1, IRAK4, GCK, Clk2, and MINK1 (IC50s = 390, 120, 430, 430, and 1,900 nM, respectively). Takinib increases caspase-3/-7 activity and inhibits proliferation of TNF-α-stimulated, but not unstimulated, MDA-MB-231 cells in a concentration-dependent manner. It reduces phosphorylation of IKK, p38 MAPK, MAPK8, MAPK9, and c-Jun in TNF-α-stimulated MDA-MB-231 cells. Takinib inhibits IL-6 secretion in TNF-α-stimulated rheumatoid arthritis fibroblast-like synoviocytes in a concentration-dependent manner. It reduces inflammation and cartilage damage in knee joints in a mouse model of collagen type II-induced arthritis when administered at a dose of 50 mg/kg per day.{57119}
Brand:CaymanSKU:24161 - 10 mgAvailable on backorder
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Takinib is a TGF-β-activated kinase 1 (TAK1) inhibitor (IC50 = 9.5 nM).{40308} It is selective for TAK1 over IRAK1, IRAK4, GCK, Clk2, and MINK1 (IC50s = 390, 120, 430, 430, and 1,900 nM, respectively). Takinib increases caspase-3/-7 activity and inhibits proliferation of TNF-α-stimulated, but not unstimulated, MDA-MB-231 cells in a concentration-dependent manner. It reduces phosphorylation of IKK, p38 MAPK, MAPK8, MAPK9, and c-Jun in TNF-α-stimulated MDA-MB-231 cells. Takinib inhibits IL-6 secretion in TNF-α-stimulated rheumatoid arthritis fibroblast-like synoviocytes in a concentration-dependent manner. It reduces inflammation and cartilage damage in knee joints in a mouse model of collagen type II-induced arthritis when administered at a dose of 50 mg/kg per day.{57119}
Brand:CaymanSKU:24161 - 25 mgAvailable on backorder
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Takinib is a TGF-β-activated kinase 1 (TAK1) inhibitor (IC50 = 9.5 nM).{40308} It is selective for TAK1 over IRAK1, IRAK4, GCK, Clk2, and MINK1 (IC50s = 390, 120, 430, 430, and 1,900 nM, respectively). Takinib increases caspase-3/-7 activity and inhibits proliferation of TNF-α-stimulated, but not unstimulated, MDA-MB-231 cells in a concentration-dependent manner. It reduces phosphorylation of IKK, p38 MAPK, MAPK8, MAPK9, and c-Jun in TNF-α-stimulated MDA-MB-231 cells. Takinib inhibits IL-6 secretion in TNF-α-stimulated rheumatoid arthritis fibroblast-like synoviocytes in a concentration-dependent manner. It reduces inflammation and cartilage damage in knee joints in a mouse model of collagen type II-induced arthritis when administered at a dose of 50 mg/kg per day.{57119}
Brand:CaymanSKU:24161 - 5 mgAvailable on backorder
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Talabostat is a non-selective inhibitor of dipeptidyl peptidases (DPPs), including DPP-4, DPP-7, DPP-8, DPP-9, fibroblast activation protein (FAP), and prolyl endopeptidase (PREP; IC50s = >4, 310, 4, 11, 560, and 390 nM, respectively).{47719} It inhibits proliferation of superantigen-stimulated human peripheral blood mononuclear cells (PBMCs; IC50 = ~10 nM). Talabostat (5 μg twice per day) increases expression of a variety of cytokines, including those encoding IL-1β, IL-6, and G-CSF, and chemokines in tumors and tumor-draining lymph nodes in a WEHI-164 fibrosarcoma mouse model.{47720} It reduces tumor growth in WEHI-164, MM45T.Sp, and MM52.T fibrosarcoma, EL-4 and A20/2J lymphoma, B16/F10 melanoma, and P815 mastocytoma syngeneic mouse models. Talabostat also increases the efficacy of the antitumor antibodies rituximab and trastuzumab in Namalwa B cell lymphoma and LS180 colon carcinoma mouse xenograft models, respectively.
Brand:CaymanSKU:29007 - 10 mgAvailable on backorder
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Talabostat is a non-selective inhibitor of dipeptidyl peptidases (DPPs), including DPP-4, DPP-7, DPP-8, DPP-9, fibroblast activation protein (FAP), and prolyl endopeptidase (PREP; IC50s = >4, 310, 4, 11, 560, and 390 nM, respectively).{47719} It inhibits proliferation of superantigen-stimulated human peripheral blood mononuclear cells (PBMCs; IC50 = ~10 nM). Talabostat (5 μg twice per day) increases expression of a variety of cytokines, including those encoding IL-1β, IL-6, and G-CSF, and chemokines in tumors and tumor-draining lymph nodes in a WEHI-164 fibrosarcoma mouse model.{47720} It reduces tumor growth in WEHI-164, MM45T.Sp, and MM52.T fibrosarcoma, EL-4 and A20/2J lymphoma, B16/F10 melanoma, and P815 mastocytoma syngeneic mouse models. Talabostat also increases the efficacy of the antitumor antibodies rituximab and trastuzumab in Namalwa B cell lymphoma and LS180 colon carcinoma mouse xenograft models, respectively.
Brand:CaymanSKU:29007 - 25 mgAvailable on backorder
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Talabostat is a non-selective inhibitor of dipeptidyl peptidases (DPPs), including DPP-4, DPP-7, DPP-8, DPP-9, fibroblast activation protein (FAP), and prolyl endopeptidase (PREP; IC50s = >4, 310, 4, 11, 560, and 390 nM, respectively).{47719} It inhibits proliferation of superantigen-stimulated human peripheral blood mononuclear cells (PBMCs; IC50 = ~10 nM). Talabostat (5 μg twice per day) increases expression of a variety of cytokines, including those encoding IL-1β, IL-6, and G-CSF, and chemokines in tumors and tumor-draining lymph nodes in a WEHI-164 fibrosarcoma mouse model.{47720} It reduces tumor growth in WEHI-164, MM45T.Sp, and MM52.T fibrosarcoma, EL-4 and A20/2J lymphoma, B16/F10 melanoma, and P815 mastocytoma syngeneic mouse models. Talabostat also increases the efficacy of the antitumor antibodies rituximab and trastuzumab in Namalwa B cell lymphoma and LS180 colon carcinoma mouse xenograft models, respectively.
Brand:CaymanSKU:29007 - 5 mgAvailable on backorder
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Talabostat is a non-selective inhibitor of dipeptidyl peptidases (DPPs), including DPP-4, DPP-7, DPP-8, DPP-9, fibroblast activation protein (FAP), and prolyl endopeptidase (PREP; IC50s = >4, 310, 4, 11, 560, and 390 nM, respectively).{47719} It inhibits proliferation of superantigen-stimulated human peripheral blood mononuclear cells (PBMCs; IC50 = ~10 nM). Talabostat (5 μg twice per day) increases expression of a variety of cytokines, including those encoding IL-1β, IL-6, and G-CSF, and chemokines in tumors and tumor-draining lymph nodes in a WEHI-164 fibrosarcoma mouse model.{47720} It reduces tumor growth in WEHI-164, MM45T.Sp, and MM52.T fibrosarcoma, EL-4 and A20/2J lymphoma, B16/F10 melanoma, and P815 mastocytoma syngeneic mouse models. Talabostat also increases the efficacy of the antitumor antibodies rituximab and trastuzumab in Namalwa B cell lymphoma and LS180 colon carcinoma mouse xenograft models, respectively.
Brand:CaymanSKU:29007 - 50 mgAvailable on backorder
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Talampanel is an allosteric AMPA receptor antagonist (IC50 = 2.5 µM in cerebellar Purkinje neurons using voltage-clamp electrophysiology).{39888} It reduces the firing rate of spinal neurons in rats by 68% when administered at a dose of 10 mg/kg following AMPA administration.{39889} It is protective against seizures in mouse models of epilepsy including maximum electroshock (MES; ED50 = 8.6 mg/kg) and 4-aminopyridine models (Item No. 18511; ED50 = 8.4 mg/kg). It also potentiates the effects of diazepam in MES- and metrazole-induced seizure models when administered at a dose of 2 mg/kg.{39890} Talampanel is neuroprotective, reducing lesion size in rat and mouse models of focal ischemia.
Brand:CaymanSKU:- -
Talampanel is an allosteric AMPA receptor antagonist (IC50 = 2.5 µM in cerebellar Purkinje neurons using voltage-clamp electrophysiology).{39888} It reduces the firing rate of spinal neurons in rats by 68% when administered at a dose of 10 mg/kg following AMPA administration.{39889} It is protective against seizures in mouse models of epilepsy including maximum electroshock (MES; ED50 = 8.6 mg/kg) and 4-aminopyridine models (Item No. 18511; ED50 = 8.4 mg/kg). It also potentiates the effects of diazepam in MES- and metrazole-induced seizure models when administered at a dose of 2 mg/kg.{39890} Talampanel is neuroprotective, reducing lesion size in rat and mouse models of focal ischemia.
Brand:CaymanSKU:- -
Talampanel is an allosteric AMPA receptor antagonist (IC50 = 2.5 µM in cerebellar Purkinje neurons using voltage-clamp electrophysiology).{39888} It reduces the firing rate of spinal neurons in rats by 68% when administered at a dose of 10 mg/kg following AMPA administration.{39889} It is protective against seizures in mouse models of epilepsy including maximum electroshock (MES; ED50 = 8.6 mg/kg) and 4-aminopyridine models (Item No. 18511; ED50 = 8.4 mg/kg). It also potentiates the effects of diazepam in MES- and metrazole-induced seizure models when administered at a dose of 2 mg/kg.{39890} Talampanel is neuroprotective, reducing lesion size in rat and mouse models of focal ischemia.
Brand:CaymanSKU:- -
Talampanel is an allosteric AMPA receptor antagonist (IC50 = 2.5 µM in cerebellar Purkinje neurons using voltage-clamp electrophysiology).{39888} It reduces the firing rate of spinal neurons in rats by 68% when administered at a dose of 10 mg/kg following AMPA administration.{39889} It is protective against seizures in mouse models of epilepsy including maximum electroshock (MES; ED50 = 8.6 mg/kg) and 4-aminopyridine models (Item No. 18511; ED50 = 8.4 mg/kg). It also potentiates the effects of diazepam in MES- and metrazole-induced seizure models when administered at a dose of 2 mg/kg.{39890} Talampanel is neuroprotective, reducing lesion size in rat and mouse models of focal ischemia.
Brand:CaymanSKU:- -
Talatisamine is a diterpene alkaloid originally isolated from A. talassicum and has diverse biological activities.{47536,47537,47538,47539,47540} It blocks delayed rectifier potassium (IK) current in rat hippocampal neurons (IC50 = 146 μM).{47538} Talatisamine reduces increases in IK current and cytotoxicity in primary rat cortical neurons induced by amyloid-β (1-40) (Aβ40; Item No. 21617).{47539} It inhibits barium chloride-induced contractions in isolated rat intenstines (EC50 = 200 μM).{47537} Talatisamine exhibits feeding deterrent activity against red flour beetle (T. castaneum) adults (EC50 = 342.8 ppm).{47540}
Brand:CaymanSKU:27721 - 10 mgAvailable on backorder
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Talatisamine is a diterpene alkaloid originally isolated from A. talassicum and has diverse biological activities.{47536,47537,47538,47539,47540} It blocks delayed rectifier potassium (IK) current in rat hippocampal neurons (IC50 = 146 μM).{47538} Talatisamine reduces increases in IK current and cytotoxicity in primary rat cortical neurons induced by amyloid-β (1-40) (Aβ40; Item No. 21617).{47539} It inhibits barium chloride-induced contractions in isolated rat intenstines (EC50 = 200 μM).{47537} Talatisamine exhibits feeding deterrent activity against red flour beetle (T. castaneum) adults (EC50 = 342.8 ppm).{47540}
Brand:CaymanSKU:27721 - 25 mgAvailable on backorder
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Talatisamine is a diterpene alkaloid originally isolated from A. talassicum and has diverse biological activities.{47536,47537,47538,47539,47540} It blocks delayed rectifier potassium (IK) current in rat hippocampal neurons (IC50 = 146 μM).{47538} Talatisamine reduces increases in IK current and cytotoxicity in primary rat cortical neurons induced by amyloid-β (1-40) (Aβ40; Item No. 21617).{47539} It inhibits barium chloride-induced contractions in isolated rat intenstines (EC50 = 200 μM).{47537} Talatisamine exhibits feeding deterrent activity against red flour beetle (T. castaneum) adults (EC50 = 342.8 ppm).{47540}
Brand:CaymanSKU:27721 - 5 mgAvailable on backorder
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Talatisamine is a diterpene alkaloid originally isolated from A. talassicum and has diverse biological activities.{47536,47537,47538,47539,47540} It blocks delayed rectifier potassium (IK) current in rat hippocampal neurons (IC50 = 146 μM).{47538} Talatisamine reduces increases in IK current and cytotoxicity in primary rat cortical neurons induced by amyloid-β (1-40) (Aβ40; Item No. 21617).{47539} It inhibits barium chloride-induced contractions in isolated rat intenstines (EC50 = 200 μM).{47537} Talatisamine exhibits feeding deterrent activity against red flour beetle (T. castaneum) adults (EC50 = 342.8 ppm).{47540}
Brand:CaymanSKU:27721 - 50 mgAvailable on backorder
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Taleranol is a β-resorcylic acid lactone and an isomer of α-zearalanol (Item No. 23424).{54232} In vivo, taleranol (1-500 µg/animal) induces synthesis of the uterine protein IP and increases uterine weight in rats.
Brand:CaymanSKU:28299 - 1 mgAvailable on backorder
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Taleranol is a β-resorcylic acid lactone and an isomer of α-zearalanol (Item No. 23424).{54232} In vivo, taleranol (1-500 µg/animal) induces synthesis of the uterine protein IP and increases uterine weight in rats.
Brand:CaymanSKU:28299 - 10 mgAvailable on backorder
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Taleranol is a β-resorcylic acid lactone and an isomer of α-zearalanol (Item No. 23424).{54232} In vivo, taleranol (1-500 µg/animal) induces synthesis of the uterine protein IP and increases uterine weight in rats.
Brand:CaymanSKU:28299 - 25 mgAvailable on backorder
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Taleranol is a β-resorcylic acid lactone and an isomer of α-zearalanol (Item No. 23424).{54232} In vivo, taleranol (1-500 µg/animal) induces synthesis of the uterine protein IP and increases uterine weight in rats.
Brand:CaymanSKU:28299 - 5 mgAvailable on backorder
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Talnetant is an antagonist of the neurokinin-3 (NK3) receptor (Ki = 1 nM).{28052} It is selective for NK3 over NK1 and NK2 receptors (Kis = 144 and >100,000 nM, respectively, in CHO cells expressing recombinant human receptors). Talnetant inhibits calcium mobilization induced by neurokinin B (Item No. 24542) in HEK293 cells expressing human NK3 receptors (IC50 = 16.6 nM). It inhibits contractions induced by the NK3 receptor agonist senktide (Item No. 16721) in isolated rabbit iris sphincter muscle (pD2 = 9.1). Talnetant (5-20 mg/kg) reduces senktide-induced head shakes and tail whips in mice. It also inhibits senktide-induced wet-dog shakes, increases extracellular dopamine and norepinephrine in the medial prefrontal cortex, and attenuates haloperidol-induced increases in nucleus accumbens dopamine levels in guinea pigs.{53729}
Brand:CaymanSKU:29699 - 100 mgAvailable on backorder
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Talnetant is an antagonist of the neurokinin-3 (NK3) receptor (Ki = 1 nM).{28052} It is selective for NK3 over NK1 and NK2 receptors (Kis = 144 and >100,000 nM, respectively, in CHO cells expressing recombinant human receptors). Talnetant inhibits calcium mobilization induced by neurokinin B (Item No. 24542) in HEK293 cells expressing human NK3 receptors (IC50 = 16.6 nM). It inhibits contractions induced by the NK3 receptor agonist senktide (Item No. 16721) in isolated rabbit iris sphincter muscle (pD2 = 9.1). Talnetant (5-20 mg/kg) reduces senktide-induced head shakes and tail whips in mice. It also inhibits senktide-induced wet-dog shakes, increases extracellular dopamine and norepinephrine in the medial prefrontal cortex, and attenuates haloperidol-induced increases in nucleus accumbens dopamine levels in guinea pigs.{53729}
Brand:CaymanSKU:29699 - 250 mgAvailable on backorder
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Talnetant is an antagonist of the neurokinin-3 (NK3) receptor (Ki = 1 nM).{28052} It is selective for NK3 over NK1 and NK2 receptors (Kis = 144 and >100,000 nM, respectively, in CHO cells expressing recombinant human receptors). Talnetant inhibits calcium mobilization induced by neurokinin B (Item No. 24542) in HEK293 cells expressing human NK3 receptors (IC50 = 16.6 nM). It inhibits contractions induced by the NK3 receptor agonist senktide (Item No. 16721) in isolated rabbit iris sphincter muscle (pD2 = 9.1). Talnetant (5-20 mg/kg) reduces senktide-induced head shakes and tail whips in mice. It also inhibits senktide-induced wet-dog shakes, increases extracellular dopamine and norepinephrine in the medial prefrontal cortex, and attenuates haloperidol-induced increases in nucleus accumbens dopamine levels in guinea pigs.{53729}
Brand:CaymanSKU:29699 - 500 mgAvailable on backorder
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Talniflumate is a prodrug form of the COX-2 inhibitor niflumic acid (Item No. 70650).{53157} It decreases the rate of chloride/bicarbonate exchange by 55% in isolated mouse intestinal villous epithelial cells when used at a concentration of 100 µM.{53158} Dietary administration of talniflumate (88 mg/kg per day) increases survival but has no effect on the number of crypt goblet cells in the jejunum or cecum in a cystic fibrosis mouse model of distal intestinal obstructive syndrome.
Brand:CaymanSKU:29623 - 10 mgAvailable on backorder
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Talniflumate is a prodrug form of the COX-2 inhibitor niflumic acid (Item No. 70650).{53157} It decreases the rate of chloride/bicarbonate exchange by 55% in isolated mouse intestinal villous epithelial cells when used at a concentration of 100 µM.{53158} Dietary administration of talniflumate (88 mg/kg per day) increases survival but has no effect on the number of crypt goblet cells in the jejunum or cecum in a cystic fibrosis mouse model of distal intestinal obstructive syndrome.
Brand:CaymanSKU:29623 - 25 mgAvailable on backorder
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Talniflumate is a prodrug form of the COX-2 inhibitor niflumic acid (Item No. 70650).{53157} It decreases the rate of chloride/bicarbonate exchange by 55% in isolated mouse intestinal villous epithelial cells when used at a concentration of 100 µM.{53158} Dietary administration of talniflumate (88 mg/kg per day) increases survival but has no effect on the number of crypt goblet cells in the jejunum or cecum in a cystic fibrosis mouse model of distal intestinal obstructive syndrome.
Brand:CaymanSKU:29623 - 5 mgAvailable on backorder
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Talniflumate is a prodrug form of the COX-2 inhibitor niflumic acid (Item No. 70650).{53157} It decreases the rate of chloride/bicarbonate exchange by 55% in isolated mouse intestinal villous epithelial cells when used at a concentration of 100 µM.{53158} Dietary administration of talniflumate (88 mg/kg per day) increases survival but has no effect on the number of crypt goblet cells in the jejunum or cecum in a cystic fibrosis mouse model of distal intestinal obstructive syndrome.
Brand:CaymanSKU:29623 - 50 mgAvailable on backorder
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There are two homologous nuclear receptors for the hormone 17β-estradiol (estrogen), commonly called ERα and ERβ. Receptor activation leads to the formation of homo- and hetero-dimers, which in turn interact with accessory proteins to regulate gene transcription. Tamoxifen is a selective estrogen receptor modulator, evoking tissue-dependent effects. It is an antagonist of ER action in breast tissue and breast cancer cells and is reported to be effective in the treatment of early breast cancer to prevent tumor growth.{17813,17814} Importantly, tamoxifen has been reported to act as an ER agonist in bone and blood vessels, helping to minimize osteoporosis and reduce the risk of cardiovascular disease in post-menopausal women.{17815} Also, tamoxifen is a partial ER agonist in uterine tissues and is reported to increase the risk of endometrial carcinoma.{17816}
Brand:CaymanSKU:- -
There are two homologous nuclear receptors for the hormone 17β-estradiol (estrogen), commonly called ERα and ERβ. Receptor activation leads to the formation of homo- and hetero-dimers, which in turn interact with accessory proteins to regulate gene transcription. Tamoxifen is a selective estrogen receptor modulator, evoking tissue-dependent effects. It is an antagonist of ER action in breast tissue and breast cancer cells and is reported to be effective in the treatment of early breast cancer to prevent tumor growth.{17813,17814} Importantly, tamoxifen has been reported to act as an ER agonist in bone and blood vessels, helping to minimize osteoporosis and reduce the risk of cardiovascular disease in post-menopausal women.{17815} Also, tamoxifen is a partial ER agonist in uterine tissues and is reported to increase the risk of endometrial carcinoma.{17816}
Brand:CaymanSKU:- -
Tamoxifen (Item No. 27190) is an analytical reference standard categorized as a selective estrogen receptor modulator (SERM).{51126} Formulations containing tamoxifen have been used by bodybuilders to prevent gynecomastia associated with anabolic steroid use.{51127} Tamoxifen has been detected as an adverse analytical finding (AAF) during anti-doping testing.{48164} This product is intended for use in analytical forensic applications. This product is also available as a general research tool (Item Nos. 13258 | 11629).
Brand:CaymanSKU:27190 - 25 mgAvailable on backorder
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There are two homologous nuclear receptors for the hormone 17β-estradiol (estrogen), commonly called ERα and ERβ. Receptor activation leads to the formation of homo- and hetero-dimers, which in turn interact with accessory proteins to regulate gene transcription. Tamoxifen is a selective estrogen receptor modulator, evoking tissue-dependent effects. It is an antagonist of ER action in breast tissue and breast cancer cells and is reported to be effective in the treatment of early breast cancer to prevent tumor growth.{17813,17814} Importantly, tamoxifen has been reported to act as an ER agonist in bone and blood vessels, helping to minimize osteoporosis and reduce the risk of cardiovascular disease in post-menopausal women.{17815} Also, tamoxifen is a partial ER agonist in uterine tissues and is reported to increase the risk of endometrial carcinoma.{17816}
Brand:CaymanSKU:- -
Tamoxifen (Item No. 27190) is an analytical reference standard categorized as a selective estrogen receptor modulator (SERM).{51126} Formulations containing tamoxifen have been used by bodybuilders to prevent gynecomastia associated with anabolic steroid use.{51127} Tamoxifen has been detected as an adverse analytical finding (AAF) during anti-doping testing.{48164} This product is intended for use in analytical forensic applications. This product is also available as a general research tool (Item Nos. 13258 | 11629).
Brand:CaymanSKU:27190 - 5 mgAvailable on backorder
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There are two homologous nuclear receptors for the hormone 17β-estradiol (estrogen), commonly called ERα and ERβ. Receptor activation leads to the formation of homo- and hetero-dimers, which in turn interact with accessory proteins to regulate gene transcription. Tamoxifen is a selective estrogen receptor modulator, evoking tissue-dependent effects. It is an antagonist of ER action in breast tissue and breast cancer cells and is reported to be effective in the treatment of early breast cancer to prevent tumor growth.{17813,17814} Importantly, tamoxifen has been reported to act as an ER agonist in bone and blood vessels, helping to minimize osteoporosis and reduce the risk of cardiovascular disease in post-menopausal women.{17815} Also, tamoxifen is a partial ER agonist in uterine tissues and is reported to increase the risk of endometrial carcinoma.{17816}
Brand:CaymanSKU:- -
Tamoxifen (TMX) is a selective estrogen receptor (ER) modulator used as adjuvant therapy for estrogen-dependent breast cancer.{17814} TMX treatment serves to increase ER activity in bone, uterus, and the cardiovasculature system as it decreases ER activity in breast tissues.{10559} TMX is metabolized by cytochrome P450 (CYP450) enzymes to the active metabolites N-desmethyl-TMX, 4-hydroxy-N-desmethyl-TMX (endoxifen), and 4-hydroxy-TMX, indicating that certain CYP450 isoforms may be crucial for some of the effects of TMX.{20776} In addition, TMX binds microsomal antiestrogen binding sites, altering cholesterol esterification at therapeutic doses and impacting breast cancer cell differentiation, apoptosis, and autophagy.{20775}
Brand:CaymanSKU:11629 - 1 gAvailable on backorder
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Tamoxifen (TMX) is a selective estrogen receptor (ER) modulator used as adjuvant therapy for estrogen-dependent breast cancer.{17814} TMX treatment serves to increase ER activity in bone, uterus, and the cardiovasculature system as it decreases ER activity in breast tissues.{10559} TMX is metabolized by cytochrome P450 (CYP450) enzymes to the active metabolites N-desmethyl-TMX, 4-hydroxy-N-desmethyl-TMX (endoxifen), and 4-hydroxy-TMX, indicating that certain CYP450 isoforms may be crucial for some of the effects of TMX.{20776} In addition, TMX binds microsomal antiestrogen binding sites, altering cholesterol esterification at therapeutic doses and impacting breast cancer cell differentiation, apoptosis, and autophagy.{20775}
Brand:CaymanSKU:11629 - 10 gAvailable on backorder
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Tamoxifen (TMX) is a selective estrogen receptor (ER) modulator used as adjuvant therapy for estrogen-dependent breast cancer.{17814} TMX treatment serves to increase ER activity in bone, uterus, and the cardiovasculature system as it decreases ER activity in breast tissues.{10559} TMX is metabolized by cytochrome P450 (CYP450) enzymes to the active metabolites N-desmethyl-TMX, 4-hydroxy-N-desmethyl-TMX (endoxifen), and 4-hydroxy-TMX, indicating that certain CYP450 isoforms may be crucial for some of the effects of TMX.{20776} In addition, TMX binds microsomal antiestrogen binding sites, altering cholesterol esterification at therapeutic doses and impacting breast cancer cell differentiation, apoptosis, and autophagy.{20775}
Brand:CaymanSKU:11629 - 5 gAvailable on backorder
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Tamoxifen (TMX) is a selective estrogen receptor (ER) modulator used as adjuvant therapy for estrogen-dependent breast cancer.{17814} TMX treatment serves to increase ER activity in bone, uterus, and the cardiovasculature system as it decreases ER activity in breast tissues.{10559} TMX is metabolized by cytochrome P450 (CYP450) enzymes to the active metabolites N-desmethyl-TMX, 4-hydroxy-N-desmethyl-TMX (endoxifen), and 4-hydroxy-TMX, indicating that certain CYP450 isoforms may be crucial for some of the effects of TMX.{20776} In addition, TMX binds microsomal antiestrogen binding sites, altering cholesterol esterification at therapeutic doses and impacting breast cancer cell differentiation, apoptosis, and autophagy.{20775}
Brand:CaymanSKU:11629 - 500 mgAvailable on backorder
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Tamoxifen (Item No. 13258) is a selective estrogen receptor modulator that evokes tissue-dependent effects.{17813,17814,17815,17816} Tamoxifen N-oxide is a metabolite of tamoxifen that is produced by the action of flavin-containing monooxygenases.{30184,30180} It can be converted back to tamoxifen by cytochrome P450 isoforms and hemoglobin.{30179,30180} Like the parent compound, tamoxifen N-oxide can form DNA adducts.{30181,30182,30184} Tamoxifen N-oxide is a weak inhibitor of human hydroxysteroid sulfotransferase 2A1 (Kis = 9.1 and 16.9 µM for the sulfonation of dehydroepiandrosterone and pregnenolone, respectively).{30183}
Brand:CaymanSKU:-Available on backorder
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Tamoxifen (Item No. 13258) is a selective estrogen receptor modulator that evokes tissue-dependent effects.{17813,17814,17815,17816} Tamoxifen N-oxide is a metabolite of tamoxifen that is produced by the action of flavin-containing monooxygenases.{30184,30180} It can be converted back to tamoxifen by cytochrome P450 isoforms and hemoglobin.{30179,30180} Like the parent compound, tamoxifen N-oxide can form DNA adducts.{30181,30182,30184} Tamoxifen N-oxide is a weak inhibitor of human hydroxysteroid sulfotransferase 2A1 (Kis = 9.1 and 16.9 µM for the sulfonation of dehydroepiandrosterone and pregnenolone, respectively).{30183}
Brand:CaymanSKU:-Available on backorder
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Tamoxifen (Item No. 13258) is a selective estrogen receptor modulator that evokes tissue-dependent effects.{17813,17814,17815,17816} Tamoxifen N-oxide is a metabolite of tamoxifen that is produced by the action of flavin-containing monooxygenases.{30184,30180} It can be converted back to tamoxifen by cytochrome P450 isoforms and hemoglobin.{30179,30180} Like the parent compound, tamoxifen N-oxide can form DNA adducts.{30181,30182,30184} Tamoxifen N-oxide is a weak inhibitor of human hydroxysteroid sulfotransferase 2A1 (Kis = 9.1 and 16.9 µM for the sulfonation of dehydroepiandrosterone and pregnenolone, respectively).{30183}
Brand:CaymanSKU:-Available on backorder
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Tamoxifen-d5 contains five deuterium atoms at the 3, 3, 4, 4, and 4 positions. It is intended for use as an internal standard for the quantification of tamoxifen (Item No. 13258) by GC- or LC-MS. Tamoxifen is a selective estrogen receptor (ER) modulator, evoking tissue-dependent effects. It is an antagonist of ER action in breast tissue and breast cancer cells and is reported to be effective in the treatment of early breast cancer to prevent tumor growth.{17813,17814} Importantly, tamoxifen has been reported to act as an ER agonist in bone and blood vessels, helping to minimize osteoporosis and reduce the risk of cardiovascular disease in post-menopausal women.{17815} Also, tamoxifen is a partial ER agonist in uterine tissues and is reported to increase the risk of endometrial carcinoma.{17816}
Brand:CaymanSKU:-Available on backorder
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Tamoxifen-d5 contains five deuterium atoms at the 3, 3, 4, 4, and 4 positions. It is intended for use as an internal standard for the quantification of tamoxifen (Item No. 13258) by GC- or LC-MS. Tamoxifen is a selective estrogen receptor (ER) modulator, evoking tissue-dependent effects. It is an antagonist of ER action in breast tissue and breast cancer cells and is reported to be effective in the treatment of early breast cancer to prevent tumor growth.{17813,17814} Importantly, tamoxifen has been reported to act as an ER agonist in bone and blood vessels, helping to minimize osteoporosis and reduce the risk of cardiovascular disease in post-menopausal women.{17815} Also, tamoxifen is a partial ER agonist in uterine tissues and is reported to increase the risk of endometrial carcinoma.{17816}
Brand:CaymanSKU:-Available on backorder
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Tamsulosin is a potent antagonist of α1-adrenergic receptors (α1-ARs; Ki = 0.229 nM in a radioligand binding assay).{36342} It is 3,800-fold selective for α1-ARs over α2-ARs (Ki = 871 nM). Tamsulosin antagonizes norepinephrine-induced contraction of isolated rabbit aorta (pA2 = 10.11) but has no effect on contraction stimulated by histamine, serotonin (Item No. 14332), angiotensin II (Item No. 17150), or prostaglandin F2α (Item No. 16010). In vivo, tamsulosin reverses the pressor effect of phenylephrine (Item Nos. 17205 | 18619) in pithed rats. It reversibly reduces fertility in male rats when administered at a dose of 0.15 mg/kg.{36343} Tamsulosin (1-100 μg/kg) also reduces prostatic pressure in a dose-dependent manner with minimal hypotensive effects in anesthetized dogs.{36344} Formulations containing tamsulosin have been used for the treatment of benign prostatic hyperplasia.
Brand:CaymanSKU:24020 - 10 mgAvailable on backorder
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Tamsulosin is a potent antagonist of α1-adrenergic receptors (α1-ARs; Ki = 0.229 nM in a radioligand binding assay).{36342} It is 3,800-fold selective for α1-ARs over α2-ARs (Ki = 871 nM). Tamsulosin antagonizes norepinephrine-induced contraction of isolated rabbit aorta (pA2 = 10.11) but has no effect on contraction stimulated by histamine, serotonin (Item No. 14332), angiotensin II (Item No. 17150), or prostaglandin F2α (Item No. 16010). In vivo, tamsulosin reverses the pressor effect of phenylephrine (Item Nos. 17205 | 18619) in pithed rats. It reversibly reduces fertility in male rats when administered at a dose of 0.15 mg/kg.{36343} Tamsulosin (1-100 μg/kg) also reduces prostatic pressure in a dose-dependent manner with minimal hypotensive effects in anesthetized dogs.{36344} Formulations containing tamsulosin have been used for the treatment of benign prostatic hyperplasia.
Brand:CaymanSKU:24020 - 25 mgAvailable on backorder
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Tamsulosin is a potent antagonist of α1-adrenergic receptors (α1-ARs; Ki = 0.229 nM in a radioligand binding assay).{36342} It is 3,800-fold selective for α1-ARs over α2-ARs (Ki = 871 nM). Tamsulosin antagonizes norepinephrine-induced contraction of isolated rabbit aorta (pA2 = 10.11) but has no effect on contraction stimulated by histamine, serotonin (Item No. 14332), angiotensin II (Item No. 17150), or prostaglandin F2α (Item No. 16010). In vivo, tamsulosin reverses the pressor effect of phenylephrine (Item Nos. 17205 | 18619) in pithed rats. It reversibly reduces fertility in male rats when administered at a dose of 0.15 mg/kg.{36343} Tamsulosin (1-100 μg/kg) also reduces prostatic pressure in a dose-dependent manner with minimal hypotensive effects in anesthetized dogs.{36344} Formulations containing tamsulosin have been used for the treatment of benign prostatic hyperplasia.
Brand:CaymanSKU:24020 - 5 mgAvailable on backorder
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Tamsulosin is a potent antagonist of α1-adrenergic receptors (α1-ARs; Ki = 0.229 nM in a radioligand binding assay).{36342} It is 3,800-fold selective for α1-ARs over α2-ARs (Ki = 871 nM). Tamsulosin antagonizes norepinephrine-induced contraction of isolated rabbit aorta (pA2 = 10.11) but has no effect on contraction stimulated by histamine, serotonin (Item No. 14332), angiotensin II (Item No. 17150), or prostaglandin F2α (Item No. 16010). In vivo, tamsulosin reverses the pressor effect of phenylephrine (Item Nos. 17205 | 18619) in pithed rats. It reversibly reduces fertility in male rats when administered at a dose of 0.15 mg/kg.{36343} Tamsulosin (1-100 μg/kg) also reduces prostatic pressure in a dose-dependent manner with minimal hypotensive effects in anesthetized dogs.{36344} Formulations containing tamsulosin have been used for the treatment of benign prostatic hyperplasia.
Brand:CaymanSKU:24020 - 50 mgAvailable on backorder
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TAN 1364B is a protein tyrosine phosphatase (PTP) inhibitor and the racemic and monomeric form of RK-682 (Item No. 19450).{46275} TAN 1364B inhibits the activity of the PTPs LMW-PTP, CDC25B, and PTP1B (IC50s = 8.6, 12.4, and 0.7 µM, respectively), but the inhibitory activity against LMW-PTP and CDC25B is blocked in the presence of magnesium. TAN 1364B forms aggregates in solution and binds to both the PTP binding site and to protein surfaces.
Brand:CaymanSKU:27964 - 2.5 mgAvailable on backorder
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TAN 1364B is a protein tyrosine phosphatase (PTP) inhibitor and the racemic and monomeric form of RK-682 (Item No. 19450).{46275} TAN 1364B inhibits the activity of the PTPs LMW-PTP, CDC25B, and PTP1B (IC50s = 8.6, 12.4, and 0.7 µM, respectively), but the inhibitory activity against LMW-PTP and CDC25B is blocked in the presence of magnesium. TAN 1364B forms aggregates in solution and binds to both the PTP binding site and to protein surfaces.
Brand:CaymanSKU:27964 - 500 µgAvailable on backorder
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TAN 420C is a hydroquinone ansamycin antibiotic originally isolated from Streptomyces.{38265} It exhibits antibacterial activity against B. brevis and M. flavus (MICs = 50 and 25 μg/mL, respectively).{38266} Additionally, it inhibits proliferation in the lymphocytic leukemia cell lines P388 and KB (ED50s = 0.34 and 3.49 μg/mL, respectively).{38265}
Brand:CaymanSKU:23149 - 2.5 mgAvailable on backorder
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TAN 420C is a hydroquinone ansamycin antibiotic originally isolated from Streptomyces.{38265} It exhibits antibacterial activity against B. brevis and M. flavus (MICs = 50 and 25 μg/mL, respectively).{38266} Additionally, it inhibits proliferation in the lymphocytic leukemia cell lines P388 and KB (ED50s = 0.34 and 3.49 μg/mL, respectively).{38265}
Brand:CaymanSKU:23149 - 500 µgAvailable on backorder
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TAN 420E is a bacterial metabolite originally isolated from Streptomyces.{38266,38265,47368} It scavenges 2,2-diphenyl-1-picrylhydrazyl (DPPH; Item No. 14805) radicals in a cell-free assay (IC50 = 1.3 μM) and reduces thiobarbituric acid reactive substances (TBARS) in rat liver microsomes by 72% when used at a concentration of 100 μg/ml.{47368} TAN 420E is active against B. brevis, B. cereus, M. flavus, and S. aureus (MICs = 50-100 μg/ml).{38266} It is cytotoxic to P388 and KB lymphocytic leukemia cells (EC50s = 0.022 and 0.3 μg/ml, respectively).{38265}
Brand:CaymanSKU:28120 - 2.5 mgAvailable on backorder
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TAN 420E is a bacterial metabolite originally isolated from Streptomyces.{38266,38265,47368} It scavenges 2,2-diphenyl-1-picrylhydrazyl (DPPH; Item No. 14805) radicals in a cell-free assay (IC50 = 1.3 μM) and reduces thiobarbituric acid reactive substances (TBARS) in rat liver microsomes by 72% when used at a concentration of 100 μg/ml.{47368} TAN 420E is active against B. brevis, B. cereus, M. flavus, and S. aureus (MICs = 50-100 μg/ml).{38266} It is cytotoxic to P388 and KB lymphocytic leukemia cells (EC50s = 0.022 and 0.3 μg/ml, respectively).{38265}
Brand:CaymanSKU:28120 - 500 µgAvailable on backorder
