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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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