Cayman
Showing 40951–41100 of 45550 results
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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 - 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
Brand:CaymanSKU:33008- 100 µl Brand:CaymanSKU:33008 - 100 µlAvailable on backorder
Brand:CaymanSKU:33008- 100 µlAvailable on backorder
Brand:CaymanSKU:33010- 100 µl Brand:CaymanSKU:33010 - 100 µlAvailable on backorder
Brand:CaymanSKU:33010- 100 µlAvailable on backorder
Brand:CaymanSKU:33037- 100 µl Brand:CaymanSKU:33037 - 100 µlAvailable on backorder
Brand:CaymanSKU:33037- 100 µlAvailable 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:-
Brand:CaymanSKU:33056- 100 µl Brand:CaymanSKU:33056 - 100 µlAvailable on backorder
Brand:CaymanSKU:33056- 100 µlAvailable 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 - 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
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-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
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
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
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
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
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
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
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
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
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
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
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
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
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
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