Cayman
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Raf-1 is a proto-oncogene serine/threonine protein kinase that signals from Ras to the MAPK/ERK signaling pathway.{14539,15155} This pathway mediates basic cellular functions, including proliferation, differentiation, and survival.{14539} GW 5074 is a potent, selective, and cell-permeable inhibitor of Raf-1 (IC50 = 9 nM).{24584} It blocks phosphorylation of ERK1/2 by 90% in cells stimulated with epidermal growth factor when given at 5 µM.{24584} GW 5074 shows more than 100-fold selectivity for Raf-1 versus several related kinases.{24584}
Brand:CaymanSKU:10010368 - 10 mgAvailable on backorder
Raf-1 is a proto-oncogene serine/threonine protein kinase that signals from Ras to the MAPK/ERK signaling pathway.{14539,15155} This pathway mediates basic cellular functions, including proliferation, differentiation, and survival.{14539} GW 5074 is a potent, selective, and cell-permeable inhibitor of Raf-1 (IC50 = 9 nM).{24584} It blocks phosphorylation of ERK1/2 by 90% in cells stimulated with epidermal growth factor when given at 5 µM.{24584} GW 5074 shows more than 100-fold selectivity for Raf-1 versus several related kinases.{24584}
Brand:CaymanSKU:10010368 - 25 mgAvailable on backorder
Raf-1 is a proto-oncogene serine/threonine protein kinase that signals from Ras to the MAPK/ERK signaling pathway.{14539,15155} This pathway mediates basic cellular functions, including proliferation, differentiation, and survival.{14539} GW 5074 is a potent, selective, and cell-permeable inhibitor of Raf-1 (IC50 = 9 nM).{24584} It blocks phosphorylation of ERK1/2 by 90% in cells stimulated with epidermal growth factor when given at 5 µM.{24584} GW 5074 shows more than 100-fold selectivity for Raf-1 versus several related kinases.{24584}
Brand:CaymanSKU:10010368 - 5 mgAvailable on backorder
The peroxisome proliferator-activated receptors (PPARs) α, γ, and δ are ligand-activated transcription factors that play a key role in lipid homeostasis. Activation of PPARα results in increased clearance of triglyceride (TG) rich very low-density lipoprotein (VLDL) via a reduction in plasma levels of ApoCIII and in upregulation of ApoA1, the principal lipoprotein component of HDL.{14733} GW 590735 is a potent and selective agonist of PPARα with an EC50 value of 4 nM for the expression a GAL4-responsive reporter gene and at least 500-fold selectivity versus PPARγ and PPARδ.{14733}
Brand:CaymanSKU:10009880 - 1 mgAvailable on backorder
The peroxisome proliferator-activated receptors (PPARs) α, γ, and δ are ligand-activated transcription factors that play a key role in lipid homeostasis. Activation of PPARα results in increased clearance of triglyceride (TG) rich very low-density lipoprotein (VLDL) via a reduction in plasma levels of ApoCIII and in upregulation of ApoA1, the principal lipoprotein component of HDL.{14733} GW 590735 is a potent and selective agonist of PPARα with an EC50 value of 4 nM for the expression a GAL4-responsive reporter gene and at least 500-fold selectivity versus PPARγ and PPARδ.{14733}
Brand:CaymanSKU:10009880 - 10 mgAvailable on backorder
The peroxisome proliferator-activated receptors (PPARs) α, γ, and δ are ligand-activated transcription factors that play a key role in lipid homeostasis. Activation of PPARα results in increased clearance of triglyceride (TG) rich very low-density lipoprotein (VLDL) via a reduction in plasma levels of ApoCIII and in upregulation of ApoA1, the principal lipoprotein component of HDL.{14733} GW 590735 is a potent and selective agonist of PPARα with an EC50 value of 4 nM for the expression a GAL4-responsive reporter gene and at least 500-fold selectivity versus PPARγ and PPARδ.{14733}
Brand:CaymanSKU:10009880 - 25 mgAvailable on backorder
The peroxisome proliferator-activated receptors (PPARs) α, γ, and δ are ligand-activated transcription factors that play a key role in lipid homeostasis. Activation of PPARα results in increased clearance of triglyceride (TG) rich very low-density lipoprotein (VLDL) via a reduction in plasma levels of ApoCIII and in upregulation of ApoA1, the principal lipoprotein component of HDL.{14733} GW 590735 is a potent and selective agonist of PPARα with an EC50 value of 4 nM for the expression a GAL4-responsive reporter gene and at least 500-fold selectivity versus PPARγ and PPARδ.{14733}
Brand:CaymanSKU:10009880 - 5 mgAvailable on backorder
GW 610 is an antitumor benzothiazole that shows growth-inhibitory activity against several cancer cell lines. In MCF-7 and MDA 468 human cancer cell lines, potent antiproliferative activity (growth inhibition (GI50) (4-aminophenyl)benzothiazoles, GW 610 is not reliant on induction of cytochrome P 1A1 (CYP1A1) expression for antitumor activity.
Brand:CaymanSKU:10008313 - 1 mgAvailable on backorder
GW 610 is an antitumor benzothiazole that shows growth-inhibitory activity against several cancer cell lines. In MCF-7 and MDA 468 human cancer cell lines, potent antiproliferative activity (growth inhibition (GI50) (4-aminophenyl)benzothiazoles, GW 610 is not reliant on induction of cytochrome P 1A1 (CYP1A1) expression for antitumor activity.
Brand:CaymanSKU:10008313 - 10 mgAvailable on backorder
GW 610 is an antitumor benzothiazole that shows growth-inhibitory activity against several cancer cell lines. In MCF-7 and MDA 468 human cancer cell lines, potent antiproliferative activity (growth inhibition (GI50) (4-aminophenyl)benzothiazoles, GW 610 is not reliant on induction of cytochrome P 1A1 (CYP1A1) expression for antitumor activity.
Brand:CaymanSKU:10008313 - 5 mgAvailable on backorder
GW 610 is an antitumor benzothiazole that shows growth-inhibitory activity against several cancer cell lines. In MCF-7 and MDA 468 human cancer cell lines, potent antiproliferative activity (growth inhibition (GI50) (4-aminophenyl)benzothiazoles, GW 610 is not reliant on induction of cytochrome P 1A1 (CYP1A1) expression for antitumor activity.
Brand:CaymanSKU:10008313 - 50 mgAvailable on backorder
The effects of prostaglandin E2 (PGE2) are transduced by at least four distinct receptors designated EP1, EP2, EP3, and EP4.{1422} GW 627368X is a potent and selective competitive antagonist of the EP4 receptor with additional human TP receptor affinity. In competition radioligand bioassays, GW 627368X had affinity for human EP4 and TP receptors with Ki values of 100 nM and 158 nM, respectively.{14284} Affinity for all other human prostanoid receptors is >5.0 µM. In human washed platelets, GW 627368X produced 100% inhibition of U-46619 (EC100)-induced aggregation at a concentration of 10 µM.
Brand:CaymanSKU:10009162 - 1 mgAvailable on backorder
The effects of prostaglandin E2 (PGE2) are transduced by at least four distinct receptors designated EP1, EP2, EP3, and EP4.{1422} GW 627368X is a potent and selective competitive antagonist of the EP4 receptor with additional human TP receptor affinity. In competition radioligand bioassays, GW 627368X had affinity for human EP4 and TP receptors with Ki values of 100 nM and 158 nM, respectively.{14284} Affinity for all other human prostanoid receptors is >5.0 µM. In human washed platelets, GW 627368X produced 100% inhibition of U-46619 (EC100)-induced aggregation at a concentration of 10 µM.
Brand:CaymanSKU:10009162 - 10 mgAvailable on backorder
The effects of prostaglandin E2 (PGE2) are transduced by at least four distinct receptors designated EP1, EP2, EP3, and EP4.{1422} GW 627368X is a potent and selective competitive antagonist of the EP4 receptor with additional human TP receptor affinity. In competition radioligand bioassays, GW 627368X had affinity for human EP4 and TP receptors with Ki values of 100 nM and 158 nM, respectively.{14284} Affinity for all other human prostanoid receptors is >5.0 µM. In human washed platelets, GW 627368X produced 100% inhibition of U-46619 (EC100)-induced aggregation at a concentration of 10 µM.
Brand:CaymanSKU:10009162 - 25 mgAvailable on backorder
The effects of prostaglandin E2 (PGE2) are transduced by at least four distinct receptors designated EP1, EP2, EP3, and EP4.{1422} GW 627368X is a potent and selective competitive antagonist of the EP4 receptor with additional human TP receptor affinity. In competition radioligand bioassays, GW 627368X had affinity for human EP4 and TP receptors with Ki values of 100 nM and 158 nM, respectively.{14284} Affinity for all other human prostanoid receptors is >5.0 µM. In human washed platelets, GW 627368X produced 100% inhibition of U-46619 (EC100)-induced aggregation at a concentration of 10 µM.
Brand:CaymanSKU:10009162 - 5 mgAvailable on backorder
The peroxisome proliferator-activated receptor α (PPARα) is a nuclear receptor that regulates the expression of genes involved in fatty acid metabolism, lipoprotein synthesis and metabolism, and inflammation.{7654,14916,20898} GW 6471 is an antagonist of PPARα (IC50 = 240 nM).{23912} It drives the displacement of coactivators from PPARα and promotes the recruitment of co-repressor proteins like nuclear co-repressor.{23912} GW 6471 is used in cell-free, cell lysate, and whole cell systems to examine the impact of PPARα antagonism.{23911,23910,23913}
Brand:CaymanSKU:11697 - 1 mgAvailable on backorder
The peroxisome proliferator-activated receptor α (PPARα) is a nuclear receptor that regulates the expression of genes involved in fatty acid metabolism, lipoprotein synthesis and metabolism, and inflammation.{7654,14916,20898} GW 6471 is an antagonist of PPARα (IC50 = 240 nM).{23912} It drives the displacement of coactivators from PPARα and promotes the recruitment of co-repressor proteins like nuclear co-repressor.{23912} GW 6471 is used in cell-free, cell lysate, and whole cell systems to examine the impact of PPARα antagonism.{23911,23910,23913}
Brand:CaymanSKU:11697 - 10 mgAvailable on backorder
The peroxisome proliferator-activated receptor α (PPARα) is a nuclear receptor that regulates the expression of genes involved in fatty acid metabolism, lipoprotein synthesis and metabolism, and inflammation.{7654,14916,20898} GW 6471 is an antagonist of PPARα (IC50 = 240 nM).{23912} It drives the displacement of coactivators from PPARα and promotes the recruitment of co-repressor proteins like nuclear co-repressor.{23912} GW 6471 is used in cell-free, cell lysate, and whole cell systems to examine the impact of PPARα antagonism.{23911,23910,23913}
Brand:CaymanSKU:11697 - 25 mgAvailable on backorder
The peroxisome proliferator-activated receptor α (PPARα) is a nuclear receptor that regulates the expression of genes involved in fatty acid metabolism, lipoprotein synthesis and metabolism, and inflammation.{7654,14916,20898} GW 6471 is an antagonist of PPARα (IC50 = 240 nM).{23912} It drives the displacement of coactivators from PPARα and promotes the recruitment of co-repressor proteins like nuclear co-repressor.{23912} GW 6471 is used in cell-free, cell lysate, and whole cell systems to examine the impact of PPARα antagonism.{23911,23910,23913}
Brand:CaymanSKU:11697 - 5 mgAvailable on backorder
Peroxisome proliferator-activated receptor-α (PPARα) is a ligand-activated transcription factor involved in the regulation of lipid homeostasis.{6374,4136} Activation of PPARα results in expression of a variety of genes, particularly those involved in fatty acid β-oxidation, binding, and transport.{11955} GW 7647 is a potent, selective agonist of human and murine PPARα{14085} It activates human PPARα, PPARγ, and PPARδ with EC50 values of 0.006, 1.1 and 6.2 µM, respectively, in a GAL4-PPAR binding assay. Similar EC50 values of 0.001, 1.3, and 2.9 were observed with the murine receptors. GW 7647 lowered triglycerides 93% and 60% in fat-fed hamsters and rats, respectively, at a dose of 3 mg/kg.{14085}
Brand:CaymanSKU:10008613 - 1 mgAvailable on backorder
Peroxisome proliferator-activated receptor-α (PPARα) is a ligand-activated transcription factor involved in the regulation of lipid homeostasis.{6374,4136} Activation of PPARα results in expression of a variety of genes, particularly those involved in fatty acid β-oxidation, binding, and transport.{11955} GW 7647 is a potent, selective agonist of human and murine PPARα{14085} It activates human PPARα, PPARγ, and PPARδ with EC50 values of 0.006, 1.1 and 6.2 µM, respectively, in a GAL4-PPAR binding assay. Similar EC50 values of 0.001, 1.3, and 2.9 were observed with the murine receptors. GW 7647 lowered triglycerides 93% and 60% in fat-fed hamsters and rats, respectively, at a dose of 3 mg/kg.{14085}
Brand:CaymanSKU:10008613 - 10 mgAvailable on backorder
Peroxisome proliferator-activated receptor-α (PPARα) is a ligand-activated transcription factor involved in the regulation of lipid homeostasis.{6374,4136} Activation of PPARα results in expression of a variety of genes, particularly those involved in fatty acid β-oxidation, binding, and transport.{11955} GW 7647 is a potent, selective agonist of human and murine PPARα{14085} It activates human PPARα, PPARγ, and PPARδ with EC50 values of 0.006, 1.1 and 6.2 µM, respectively, in a GAL4-PPAR binding assay. Similar EC50 values of 0.001, 1.3, and 2.9 were observed with the murine receptors. GW 7647 lowered triglycerides 93% and 60% in fat-fed hamsters and rats, respectively, at a dose of 3 mg/kg.{14085}
Brand:CaymanSKU:10008613 - 25 mgAvailable on backorder
Peroxisome proliferator-activated receptor-α (PPARα) is a ligand-activated transcription factor involved in the regulation of lipid homeostasis.{6374,4136} Activation of PPARα results in expression of a variety of genes, particularly those involved in fatty acid β-oxidation, binding, and transport.{11955} GW 7647 is a potent, selective agonist of human and murine PPARα{14085} It activates human PPARα, PPARγ, and PPARδ with EC50 values of 0.006, 1.1 and 6.2 µM, respectively, in a GAL4-PPAR binding assay. Similar EC50 values of 0.001, 1.3, and 2.9 were observed with the murine receptors. GW 7647 lowered triglycerides 93% and 60% in fat-fed hamsters and rats, respectively, at a dose of 3 mg/kg.{14085}
Brand:CaymanSKU:10008613 - 5 mgAvailable on backorder
GW 766994 is an antagonist of chemokine (C-C motif) receptor 3 (CCR3) with a Ki value of 13.8 nM in an assay of eosinophil chemotaxis induced by chemokine (C-C motif) ligand 11 (CCL11).{50126} It decreases CCL11-induced cyclin-dependent kinase 5 (Cdk5) and tau phosphorylation and production of amyloid β (1-42) (Aβ42) in isolated mouse hippocampal neurons when used at a concentration of 10 µM.{50127}
Brand:CaymanSKU:28431 - 1 mgAvailable on backorder
GW 766994 is an antagonist of chemokine (C-C motif) receptor 3 (CCR3) with a Ki value of 13.8 nM in an assay of eosinophil chemotaxis induced by chemokine (C-C motif) ligand 11 (CCL11).{50126} It decreases CCL11-induced cyclin-dependent kinase 5 (Cdk5) and tau phosphorylation and production of amyloid β (1-42) (Aβ42) in isolated mouse hippocampal neurons when used at a concentration of 10 µM.{50127}
Brand:CaymanSKU:28431 - 5 mgAvailable on backorder
GW 788388 is a selective inhibitor of transforming growth factor-β (TGF-β) type 1 receptor (TGFBR1 or ALK5; IC50 = 18 nM).{27870} It inhibits the expression of collagen type I in cells (IC50 = 93 nM) and in mice when given orally at 10 mg/kg once a day.{27870} As TGF-β stimulates fibrosis in a range of tissues, GW 788388 reduces typical features of fibrosis, including tissue remodeling, increased expression of α-smooth muscle actin and production of collagen I.{27872,27874,27875} GW 788388 also blocks TGF-β-mediated production of VEGF by fibroblasts, as well as subsequent angiogenesis in vitro.{27873} Inhibition of ALK5 signaling by GW 788388 also induces hypertrophy in femoral growth plates in rats.{27871}
Brand:CaymanSKU:- GW 788388 is a selective inhibitor of transforming growth factor-β (TGF-β) type 1 receptor (TGFBR1 or ALK5; IC50 = 18 nM).{27870} It inhibits the expression of collagen type I in cells (IC50 = 93 nM) and in mice when given orally at 10 mg/kg once a day.{27870} As TGF-β stimulates fibrosis in a range of tissues, GW 788388 reduces typical features of fibrosis, including tissue remodeling, increased expression of α-smooth muscle actin and production of collagen I.{27872,27874,27875} GW 788388 also blocks TGF-β-mediated production of VEGF by fibroblasts, as well as subsequent angiogenesis in vitro.{27873} Inhibition of ALK5 signaling by GW 788388 also induces hypertrophy in femoral growth plates in rats.{27871}
Brand:CaymanSKU:- GW 788388 is a selective inhibitor of transforming growth factor-β (TGF-β) type 1 receptor (TGFBR1 or ALK5; IC50 = 18 nM).{27870} It inhibits the expression of collagen type I in cells (IC50 = 93 nM) and in mice when given orally at 10 mg/kg once a day.{27870} As TGF-β stimulates fibrosis in a range of tissues, GW 788388 reduces typical features of fibrosis, including tissue remodeling, increased expression of α-smooth muscle actin and production of collagen I.{27872,27874,27875} GW 788388 also blocks TGF-β-mediated production of VEGF by fibroblasts, as well as subsequent angiogenesis in vitro.{27873} Inhibition of ALK5 signaling by GW 788388 also induces hypertrophy in femoral growth plates in rats.{27871}
Brand:CaymanSKU:- GW 788388 is a selective inhibitor of transforming growth factor-β (TGF-β) type 1 receptor (TGFBR1 or ALK5; IC50 = 18 nM).{27870} It inhibits the expression of collagen type I in cells (IC50 = 93 nM) and in mice when given orally at 10 mg/kg once a day.{27870} As TGF-β stimulates fibrosis in a range of tissues, GW 788388 reduces typical features of fibrosis, including tissue remodeling, increased expression of α-smooth muscle actin and production of collagen I.{27872,27874,27875} GW 788388 also blocks TGF-β-mediated production of VEGF by fibroblasts, as well as subsequent angiogenesis in vitro.{27873} Inhibition of ALK5 signaling by GW 788388 also induces hypertrophy in femoral growth plates in rats.{27871}
Brand:CaymanSKU:-
GW 803430 is an antagonist of melanin-concentrating hormone receptor 1 (MCH1; IC50 = 0.5 nM).{45224} It reduces cumulative body weight and food intake in diet-induced obese rats when administered at doses of 1 and 3 mg/kg.{45225} GW 803430 (10 and 30 mg/kg) decreases marble-burying behavior in mice, indicating anxiolytic activity, but does not affect performance in the rotorod test. It also reduces immobility time in the forced swim and tail suspension tests in mice at doses of 3 and 10 mg/kg, respectively, indicating antidepressant-like activity.
Brand:CaymanSKU:- GW 803430 is an antagonist of melanin-concentrating hormone receptor 1 (MCH1; IC50 = 0.5 nM).{45224} It reduces cumulative body weight and food intake in diet-induced obese rats when administered at doses of 1 and 3 mg/kg.{45225} GW 803430 (10 and 30 mg/kg) decreases marble-burying behavior in mice, indicating anxiolytic activity, but does not affect performance in the rotorod test. It also reduces immobility time in the forced swim and tail suspension tests in mice at doses of 3 and 10 mg/kg, respectively, indicating antidepressant-like activity.
Brand:CaymanSKU:- GW 803430 is an antagonist of melanin-concentrating hormone receptor 1 (MCH1; IC50 = 0.5 nM).{45224} It reduces cumulative body weight and food intake in diet-induced obese rats when administered at doses of 1 and 3 mg/kg.{45225} GW 803430 (10 and 30 mg/kg) decreases marble-burying behavior in mice, indicating anxiolytic activity, but does not affect performance in the rotorod test. It also reduces immobility time in the forced swim and tail suspension tests in mice at doses of 3 and 10 mg/kg, respectively, indicating antidepressant-like activity.
Brand:CaymanSKU:- GW 803430 is an antagonist of melanin-concentrating hormone receptor 1 (MCH1; IC50 = 0.5 nM).{45224} It reduces cumulative body weight and food intake in diet-induced obese rats when administered at doses of 1 and 3 mg/kg.{45225} GW 803430 (10 and 30 mg/kg) decreases marble-burying behavior in mice, indicating anxiolytic activity, but does not affect performance in the rotorod test. It also reduces immobility time in the forced swim and tail suspension tests in mice at doses of 3 and 10 mg/kg, respectively, indicating antidepressant-like activity.
Brand:CaymanSKU:-
The peripheral cannabinoid (CB2) receptor is a G protein-coupled receptor (GPCR) that is localized predominantly in immune cells, monocytes, macrophages, and in several peripheral organs and binds the active component of cannabis, Δ9-tetrahydrocannabinol, as well as anandamide, an endogenous CB receptor ligand.{15353} GW 842166X is a peripheral cannabinoid (CB2) receptor agonist with ED50 values of 91 and 63 nM in rat and human, respectively.{14965} When administered orally to rats in the Freund’s complete adjuvant (FCA) model of inflammatory pain, GW 842166X is highly potent with an ED50 value of 0.1 mg/kg and full reversal of hyperalgesia at 0.3 mg/kg.{14965}
Brand:CaymanSKU:10010372 - 1 mgAvailable on backorder
The peripheral cannabinoid (CB2) receptor is a G protein-coupled receptor (GPCR) that is localized predominantly in immune cells, monocytes, macrophages, and in several peripheral organs and binds the active component of cannabis, Δ9-tetrahydrocannabinol, as well as anandamide, an endogenous CB receptor ligand.{15353} GW 842166X is a peripheral cannabinoid (CB2) receptor agonist with ED50 values of 91 and 63 nM in rat and human, respectively.{14965} When administered orally to rats in the Freund’s complete adjuvant (FCA) model of inflammatory pain, GW 842166X is highly potent with an ED50 value of 0.1 mg/kg and full reversal of hyperalgesia at 0.3 mg/kg.{14965}
Brand:CaymanSKU:10010372 - 10 mgAvailable on backorder
The peripheral cannabinoid (CB2) receptor is a G protein-coupled receptor (GPCR) that is localized predominantly in immune cells, monocytes, macrophages, and in several peripheral organs and binds the active component of cannabis, Δ9-tetrahydrocannabinol, as well as anandamide, an endogenous CB receptor ligand.{15353} GW 842166X is a peripheral cannabinoid (CB2) receptor agonist with ED50 values of 91 and 63 nM in rat and human, respectively.{14965} When administered orally to rats in the Freund’s complete adjuvant (FCA) model of inflammatory pain, GW 842166X is highly potent with an ED50 value of 0.1 mg/kg and full reversal of hyperalgesia at 0.3 mg/kg.{14965}
Brand:CaymanSKU:10010372 - 25 mgAvailable on backorder
The peripheral cannabinoid (CB2) receptor is a G protein-coupled receptor (GPCR) that is localized predominantly in immune cells, monocytes, macrophages, and in several peripheral organs and binds the active component of cannabis, Δ9-tetrahydrocannabinol, as well as anandamide, an endogenous CB receptor ligand.{15353} GW 842166X is a peripheral cannabinoid (CB2) receptor agonist with ED50 values of 91 and 63 nM in rat and human, respectively.{14965} When administered orally to rats in the Freund’s complete adjuvant (FCA) model of inflammatory pain, GW 842166X is highly potent with an ED50 value of 0.1 mg/kg and full reversal of hyperalgesia at 0.3 mg/kg.{14965}
Brand:CaymanSKU:10010372 - 5 mgAvailable on backorder
Four G protein-coupled receptors, EP1-4, initiate cellular signaling in response to prostaglandin PGE2. The receptor EP1 acts via Gαq to evoke diverse effects, including renal vasoconstriction, bronchoconstriction, hyperalgesia, allodynia, gastric protection, hyperthermia, and sleep inhibition. GW 848687X is a potent and selective EP1 receptor antagonist (IC50 = 2.5 nM).{14997} It has >400-fold selectivity for EP1 relative to the other EP receptor subtypes, the PGD2 receptor, DP1, and the prostacyclin receptor, IP. GW 848687X is a potent and selective EP1 receptor antagonist (IC50 = 2.5 nM).{14997} It has >400-fold selectivity for EP1 relative to the other EP receptor subtypes, the PGD2 receptor, DP1, and the prostacyclin receptor, IP. GW 848687X has 30-fold selectivity over the thromboxane A2 receptor, TP, acting as a functional antagonist at this receptor at higher levels.{14997} Its actions against the FP and CRTH2/DP2 receptors have not been characterized. In vivo, GW 848687X has an excellent oral pharmacokinetic profile, with oral bioavailability at 54% in rats and 53% in dogs with a half-life of two hours in both species.{14997} In a rat model of chronic inflammatory joint pain, GW 848687X shows complete anti-hyperalgesic activity with an ED50 value of 1.3 mg/kg.{14997}
Brand:CaymanSKU:10010410 - 1 mgAvailable on backorder
Four G protein-coupled receptors, EP1-4, initiate cellular signaling in response to prostaglandin PGE2. The receptor EP1 acts via Gαq to evoke diverse effects, including renal vasoconstriction, bronchoconstriction, hyperalgesia, allodynia, gastric protection, hyperthermia, and sleep inhibition. GW 848687X is a potent and selective EP1 receptor antagonist (IC50 = 2.5 nM).{14997} It has >400-fold selectivity for EP1 relative to the other EP receptor subtypes, the PGD2 receptor, DP1, and the prostacyclin receptor, IP. GW 848687X is a potent and selective EP1 receptor antagonist (IC50 = 2.5 nM).{14997} It has >400-fold selectivity for EP1 relative to the other EP receptor subtypes, the PGD2 receptor, DP1, and the prostacyclin receptor, IP. GW 848687X has 30-fold selectivity over the thromboxane A2 receptor, TP, acting as a functional antagonist at this receptor at higher levels.{14997} Its actions against the FP and CRTH2/DP2 receptors have not been characterized. In vivo, GW 848687X has an excellent oral pharmacokinetic profile, with oral bioavailability at 54% in rats and 53% in dogs with a half-life of two hours in both species.{14997} In a rat model of chronic inflammatory joint pain, GW 848687X shows complete anti-hyperalgesic activity with an ED50 value of 1.3 mg/kg.{14997}
Brand:CaymanSKU:10010410 - 5 mgAvailable on backorder
Four G protein-coupled receptors, EP1-4, initiate cellular signaling in response to prostaglandin PGE2. The receptor EP1 acts via Gαq to evoke diverse effects, including renal vasoconstriction, bronchoconstriction, hyperalgesia, allodynia, gastric protection, hyperthermia, and sleep inhibition. GW 848687X is a potent and selective EP1 receptor antagonist (IC50 = 2.5 nM).{14997} It has >400-fold selectivity for EP1 relative to the other EP receptor subtypes, the PGD2 receptor, DP1, and the prostacyclin receptor, IP. GW 848687X is a potent and selective EP1 receptor antagonist (IC50 = 2.5 nM).{14997} It has >400-fold selectivity for EP1 relative to the other EP receptor subtypes, the PGD2 receptor, DP1, and the prostacyclin receptor, IP. GW 848687X has 30-fold selectivity over the thromboxane A2 receptor, TP, acting as a functional antagonist at this receptor at higher levels.{14997} Its actions against the FP and CRTH2/DP2 receptors have not been characterized. In vivo, GW 848687X has an excellent oral pharmacokinetic profile, with oral bioavailability at 54% in rats and 53% in dogs with a half-life of two hours in both species.{14997} In a rat model of chronic inflammatory joint pain, GW 848687X shows complete anti-hyperalgesic activity with an ED50 value of 1.3 mg/kg.{14997}
Brand:CaymanSKU:10010410 - 500 µgAvailable on backorder
GW 856553X is a selective inhibitor of p38α and p38β MAPK (pKi = 8.1 and 7.6, respectively in isolated enzyme assays).{34614} It inhibits TNF-α production (IC50 = 31 nM) in human peripheral blood mononuclear cells.{34615} It improves survival and normalizes blood pressure in rats with hypertension induced by a high salt and fat diet.{34614} It also has positive effects on cardiac remodeling and reduces HDL, LDL, and triglycerides in rats. In a clinical trial of patients with acute myocardial infarction, GW 856553X did not reduce the risk of major ischemic cardiovascular events.{34616}
Brand:CaymanSKU:- GW 856553X is a selective inhibitor of p38α and p38β MAPK (pKi = 8.1 and 7.6, respectively in isolated enzyme assays).{34614} It inhibits TNF-α production (IC50 = 31 nM) in human peripheral blood mononuclear cells.{34615} It improves survival and normalizes blood pressure in rats with hypertension induced by a high salt and fat diet.{34614} It also has positive effects on cardiac remodeling and reduces HDL, LDL, and triglycerides in rats. In a clinical trial of patients with acute myocardial infarction, GW 856553X did not reduce the risk of major ischemic cardiovascular events.{34616}
Brand:CaymanSKU:- GW 856553X is a selective inhibitor of p38α and p38β MAPK (pKi = 8.1 and 7.6, respectively in isolated enzyme assays).{34614} It inhibits TNF-α production (IC50 = 31 nM) in human peripheral blood mononuclear cells.{34615} It improves survival and normalizes blood pressure in rats with hypertension induced by a high salt and fat diet.{34614} It also has positive effects on cardiac remodeling and reduces HDL, LDL, and triglycerides in rats. In a clinical trial of patients with acute myocardial infarction, GW 856553X did not reduce the risk of major ischemic cardiovascular events.{34616}
Brand:CaymanSKU:- GW 856553X is a selective inhibitor of p38α and p38β MAPK (pKi = 8.1 and 7.6, respectively in isolated enzyme assays).{34614} It inhibits TNF-α production (IC50 = 31 nM) in human peripheral blood mononuclear cells.{34615} It improves survival and normalizes blood pressure in rats with hypertension induced by a high salt and fat diet.{34614} It also has positive effects on cardiac remodeling and reduces HDL, LDL, and triglycerides in rats. In a clinical trial of patients with acute myocardial infarction, GW 856553X did not reduce the risk of major ischemic cardiovascular events.{34616}
Brand:CaymanSKU:-
GW 9508 is a small-molecule agonist of GPR40/FFA1 (EC50 = 47.8 nM for calcium mobilization in HEK293 cells).{14194} It is selective for GPR40/FFA1 over GPR120/FFA4 (EC50 = 3,467 nM), as well as GPR43/FFA2 and GPR41/FFA3 (EC50s = >50 µM).{14194} GW 9508 potentiates glucose-stimulated and potassium chloride-mediated insulin secretion in MIN6 pancreatic β-cells but does not affect glucose-stimulated insulin secretion in primary rat or mouse islet cells.{14194} It increases phosphorylation of AMP-activated protein kinase (AMPK) and acyl-CoA carboxylase (ACC), indicating AMPK and ACC activation, and decreases hepatic lipid accumulation in a mouse model of high-cholesterol diet-induced hepatic steatosis when administered at a dose of 100 mg/kg per day for three days.{43588}
Brand:CaymanSKU:10008907 - 10 mgAvailable on backorder
GW 9508 is a small-molecule agonist of GPR40/FFA1 (EC50 = 47.8 nM for calcium mobilization in HEK293 cells).{14194} It is selective for GPR40/FFA1 over GPR120/FFA4 (EC50 = 3,467 nM), as well as GPR43/FFA2 and GPR41/FFA3 (EC50s = >50 µM).{14194} GW 9508 potentiates glucose-stimulated and potassium chloride-mediated insulin secretion in MIN6 pancreatic β-cells but does not affect glucose-stimulated insulin secretion in primary rat or mouse islet cells.{14194} It increases phosphorylation of AMP-activated protein kinase (AMPK) and acyl-CoA carboxylase (ACC), indicating AMPK and ACC activation, and decreases hepatic lipid accumulation in a mouse model of high-cholesterol diet-induced hepatic steatosis when administered at a dose of 100 mg/kg per day for three days.{43588}
Brand:CaymanSKU:10008907 - 100 mgAvailable on backorder
GW 9508 is a small-molecule agonist of GPR40/FFA1 (EC50 = 47.8 nM for calcium mobilization in HEK293 cells).{14194} It is selective for GPR40/FFA1 over GPR120/FFA4 (EC50 = 3,467 nM), as well as GPR43/FFA2 and GPR41/FFA3 (EC50s = >50 µM).{14194} GW 9508 potentiates glucose-stimulated and potassium chloride-mediated insulin secretion in MIN6 pancreatic β-cells but does not affect glucose-stimulated insulin secretion in primary rat or mouse islet cells.{14194} It increases phosphorylation of AMP-activated protein kinase (AMPK) and acyl-CoA carboxylase (ACC), indicating AMPK and ACC activation, and decreases hepatic lipid accumulation in a mouse model of high-cholesterol diet-induced hepatic steatosis when administered at a dose of 100 mg/kg per day for three days.{43588}
Brand:CaymanSKU:10008907 - 5 mgAvailable on backorder
GW 9508 is a small-molecule agonist of GPR40/FFA1 (EC50 = 47.8 nM for calcium mobilization in HEK293 cells).{14194} It is selective for GPR40/FFA1 over GPR120/FFA4 (EC50 = 3,467 nM), as well as GPR43/FFA2 and GPR41/FFA3 (EC50s = >50 µM).{14194} GW 9508 potentiates glucose-stimulated and potassium chloride-mediated insulin secretion in MIN6 pancreatic β-cells but does not affect glucose-stimulated insulin secretion in primary rat or mouse islet cells.{14194} It increases phosphorylation of AMP-activated protein kinase (AMPK) and acyl-CoA carboxylase (ACC), indicating AMPK and ACC activation, and decreases hepatic lipid accumulation in a mouse model of high-cholesterol diet-induced hepatic steatosis when administered at a dose of 100 mg/kg per day for three days.{43588}
Brand:CaymanSKU:10008907 - 50 mgAvailable on backorder
Peroxisome proliferator-activated receptor α (PPARα) is a ligand-activated transcription factor found predominantly in the liver that is involved in the regulation of lipid homeostasis.{6374,4136} Activation of PPARα results in expression of a variety of genes, particularly those involved in fatty acid β-oxidation, binding, and transport. {11955} GW 9578 is a potent agonist of PPARα that activates the murine and human receptors with EC50 values of 0.005 and 0.05 µM, respectively.{7768} GW 9578 is highly selective for PPARα compared to PPARγ and PPARδ, which it activates in murine at EC50 values of 0.15 and 2.6 µM, respectively and in human at 1.0 and 1.4 µM, respectively.{7768} GW 9578 is a potent lipid lowering agent that may reduce insulin resistance. When 0.2 mg/kg GW 9578 was given orally once daily for three days, serum total LDL cholesterol was decreased 40-60% in male Sprague-Dawely rats.{7768} Obese Zucker rats treated with 5 mg/kg GW 9578 for nine days had markedly reduced serum insulin concentrations compared to controls.{8548}
Brand:CaymanSKU:10011211 - 1 mgAvailable on backorder
Peroxisome proliferator-activated receptor α (PPARα) is a ligand-activated transcription factor found predominantly in the liver that is involved in the regulation of lipid homeostasis.{6374,4136} Activation of PPARα results in expression of a variety of genes, particularly those involved in fatty acid β-oxidation, binding, and transport. {11955} GW 9578 is a potent agonist of PPARα that activates the murine and human receptors with EC50 values of 0.005 and 0.05 µM, respectively.{7768} GW 9578 is highly selective for PPARα compared to PPARγ and PPARδ, which it activates in murine at EC50 values of 0.15 and 2.6 µM, respectively and in human at 1.0 and 1.4 µM, respectively.{7768} GW 9578 is a potent lipid lowering agent that may reduce insulin resistance. When 0.2 mg/kg GW 9578 was given orally once daily for three days, serum total LDL cholesterol was decreased 40-60% in male Sprague-Dawely rats.{7768} Obese Zucker rats treated with 5 mg/kg GW 9578 for nine days had markedly reduced serum insulin concentrations compared to controls.{8548}
Brand:CaymanSKU:10011211 - 10 mgAvailable on backorder
Peroxisome proliferator-activated receptor α (PPARα) is a ligand-activated transcription factor found predominantly in the liver that is involved in the regulation of lipid homeostasis.{6374,4136} Activation of PPARα results in expression of a variety of genes, particularly those involved in fatty acid β-oxidation, binding, and transport. {11955} GW 9578 is a potent agonist of PPARα that activates the murine and human receptors with EC50 values of 0.005 and 0.05 µM, respectively.{7768} GW 9578 is highly selective for PPARα compared to PPARγ and PPARδ, which it activates in murine at EC50 values of 0.15 and 2.6 µM, respectively and in human at 1.0 and 1.4 µM, respectively.{7768} GW 9578 is a potent lipid lowering agent that may reduce insulin resistance. When 0.2 mg/kg GW 9578 was given orally once daily for three days, serum total LDL cholesterol was decreased 40-60% in male Sprague-Dawely rats.{7768} Obese Zucker rats treated with 5 mg/kg GW 9578 for nine days had markedly reduced serum insulin concentrations compared to controls.{8548}
Brand:CaymanSKU:10011211 - 5 mgAvailable on backorder
Peroxisome proliferator-activated receptor α (PPARα) is a ligand-activated transcription factor found predominantly in the liver that is involved in the regulation of lipid homeostasis.{6374,4136} Activation of PPARα results in expression of a variety of genes, particularly those involved in fatty acid β-oxidation, binding, and transport. {11955} GW 9578 is a potent agonist of PPARα that activates the murine and human receptors with EC50 values of 0.005 and 0.05 µM, respectively.{7768} GW 9578 is highly selective for PPARα compared to PPARγ and PPARδ, which it activates in murine at EC50 values of 0.15 and 2.6 µM, respectively and in human at 1.0 and 1.4 µM, respectively.{7768} GW 9578 is a potent lipid lowering agent that may reduce insulin resistance. When 0.2 mg/kg GW 9578 was given orally once daily for three days, serum total LDL cholesterol was decreased 40-60% in male Sprague-Dawely rats.{7768} Obese Zucker rats treated with 5 mg/kg GW 9578 for nine days had markedly reduced serum insulin concentrations compared to controls.{8548}
Brand:CaymanSKU:10011211 - 500 µgAvailable on backorder
The peroxisome proliferator-activated receptor γ (PPARγ) is the nuclear receptor responsible for transducing the therapeutic activity of the thiazolidinediones. Thiazolidinediones are a group of structurally related synthetic PPARγ agonists with antidiabetic actions in vivo.{7575,8224} Rosiglitazone (BRL 49653) is a prototypical thiazolidinedione and has served as a reference compound for this class.{8241} There are many PPARγ agonists, including 15-deoxy-Δ12,14-prostaglandin J2 and azelaoyl PAF, which are naturally derived.{8461,8930} However, only a few antagonists have been reported.{8953} GW 9662 blocks the PPARγ-induced differentiation of monocytes to osteoclasts by >90% at a dose of 0.1 µM.{8953} It is therefore a much more potent antagonist than BADGE, which is another reported PPARγ antagonist.{9318}
Brand:CaymanSKU:70785 - 1 mgAvailable on backorder
The peroxisome proliferator-activated receptor γ (PPARγ) is the nuclear receptor responsible for transducing the therapeutic activity of the thiazolidinediones. Thiazolidinediones are a group of structurally related synthetic PPARγ agonists with antidiabetic actions in vivo.{7575,8224} Rosiglitazone (BRL 49653) is a prototypical thiazolidinedione and has served as a reference compound for this class.{8241} There are many PPARγ agonists, including 15-deoxy-Δ12,14-prostaglandin J2 and azelaoyl PAF, which are naturally derived.{8461,8930} However, only a few antagonists have been reported.{8953} GW 9662 blocks the PPARγ-induced differentiation of monocytes to osteoclasts by >90% at a dose of 0.1 µM.{8953} It is therefore a much more potent antagonist than BADGE, which is another reported PPARγ antagonist.{9318}
Brand:CaymanSKU:70785 - 10 mgAvailable on backorder
The peroxisome proliferator-activated receptor γ (PPARγ) is the nuclear receptor responsible for transducing the therapeutic activity of the thiazolidinediones. Thiazolidinediones are a group of structurally related synthetic PPARγ agonists with antidiabetic actions in vivo.{7575,8224} Rosiglitazone (BRL 49653) is a prototypical thiazolidinedione and has served as a reference compound for this class.{8241} There are many PPARγ agonists, including 15-deoxy-Δ12,14-prostaglandin J2 and azelaoyl PAF, which are naturally derived.{8461,8930} However, only a few antagonists have been reported.{8953} GW 9662 blocks the PPARγ-induced differentiation of monocytes to osteoclasts by >90% at a dose of 0.1 µM.{8953} It is therefore a much more potent antagonist than BADGE, which is another reported PPARγ antagonist.{9318}
Brand:CaymanSKU:70785 - 5 mgAvailable on backorder
The peroxisome proliferator-activated receptor γ (PPARγ) is the nuclear receptor responsible for transducing the therapeutic activity of the thiazolidinediones. Thiazolidinediones are a group of structurally related synthetic PPARγ agonists with antidiabetic actions in vivo.{7575,8224} Rosiglitazone (BRL 49653) is a prototypical thiazolidinedione and has served as a reference compound for this class.{8241} There are many PPARγ agonists, including 15-deoxy-Δ12,14-prostaglandin J2 and azelaoyl PAF, which are naturally derived.{8461,8930} However, only a few antagonists have been reported.{8953} GW 9662 blocks the PPARγ-induced differentiation of monocytes to osteoclasts by >90% at a dose of 0.1 µM.{8953} It is therefore a much more potent antagonist than BADGE, which is another reported PPARγ antagonist.{9318}
Brand:CaymanSKU:70785 - 50 mgAvailable on backorder
GW843682X is a reversible, cell-permeable polo-like kinase (PLK) inhibitor.{42972} It selectively inhibits Plk1 and Plk3 (IC50s = 2.2 and 9.1 nM, respectively) over PDGFR1β, VEGFR2, Aurora A, and Cdk2/cyclin A (IC50s = 160, 360, 4,800, and 7,600 nM, respectively), as well as over 30 other kinases, in a cell-free assay. GW843682X also inhibits Plk1 activity in vitro in HeLa cells (IC50 = 0.14 μM in a reporter assay using chimeric Plk1). It inhibits growth in nine cancer cell lines in a panel (IC50s = 0.11-0.7 μM) but not of PC3 human prostate cancer cells (IC50 = 6.82 µM) or non-cancerous human diploid fibroblasts (HDFs; IC50 = 6.14 μM). GW843682X inhibits growth of MES-SA human uterine sarcoma cells, as well as of the drug-resistant, P-glycoprotein-expressing MES-SA/Dx5 subline (IC50s = 0.21 and 0.21 μM, respectively). It also inhibits the growth of patient-derived leukemia cells (IC50s = 2/M cell cycle arrest and apoptosis of H460 human lung and PALL-2 and MOLM13 human leukemia cancer cells in a concentration-dependent manner.{42972,42973}
Brand:CaymanSKU:28759 - 1 mgAvailable on backorder
GW843682X is a reversible, cell-permeable polo-like kinase (PLK) inhibitor.{42972} It selectively inhibits Plk1 and Plk3 (IC50s = 2.2 and 9.1 nM, respectively) over PDGFR1β, VEGFR2, Aurora A, and Cdk2/cyclin A (IC50s = 160, 360, 4,800, and 7,600 nM, respectively), as well as over 30 other kinases, in a cell-free assay. GW843682X also inhibits Plk1 activity in vitro in HeLa cells (IC50 = 0.14 μM in a reporter assay using chimeric Plk1). It inhibits growth in nine cancer cell lines in a panel (IC50s = 0.11-0.7 μM) but not of PC3 human prostate cancer cells (IC50 = 6.82 µM) or non-cancerous human diploid fibroblasts (HDFs; IC50 = 6.14 μM). GW843682X inhibits growth of MES-SA human uterine sarcoma cells, as well as of the drug-resistant, P-glycoprotein-expressing MES-SA/Dx5 subline (IC50s = 0.21 and 0.21 μM, respectively). It also inhibits the growth of patient-derived leukemia cells (IC50s = 2/M cell cycle arrest and apoptosis of H460 human lung and PALL-2 and MOLM13 human leukemia cancer cells in a concentration-dependent manner.{42972,42973}
Brand:CaymanSKU:28759 - 10 mgAvailable on backorder
GW843682X is a reversible, cell-permeable polo-like kinase (PLK) inhibitor.{42972} It selectively inhibits Plk1 and Plk3 (IC50s = 2.2 and 9.1 nM, respectively) over PDGFR1β, VEGFR2, Aurora A, and Cdk2/cyclin A (IC50s = 160, 360, 4,800, and 7,600 nM, respectively), as well as over 30 other kinases, in a cell-free assay. GW843682X also inhibits Plk1 activity in vitro in HeLa cells (IC50 = 0.14 μM in a reporter assay using chimeric Plk1). It inhibits growth in nine cancer cell lines in a panel (IC50s = 0.11-0.7 μM) but not of PC3 human prostate cancer cells (IC50 = 6.82 µM) or non-cancerous human diploid fibroblasts (HDFs; IC50 = 6.14 μM). GW843682X inhibits growth of MES-SA human uterine sarcoma cells, as well as of the drug-resistant, P-glycoprotein-expressing MES-SA/Dx5 subline (IC50s = 0.21 and 0.21 μM, respectively). It also inhibits the growth of patient-derived leukemia cells (IC50s = 2/M cell cycle arrest and apoptosis of H460 human lung and PALL-2 and MOLM13 human leukemia cancer cells in a concentration-dependent manner.{42972,42973}
Brand:CaymanSKU:28759 - 5 mgAvailable on backorder
Gymnemagenin is the aglycone core of gymnemic acids A and B, triterpenoid sweetness inhibitors derived from G. sylvestre.{39213} It is used as a biomarker for the quantification of gymnemic acids in medicinal plant extracts.{39214}
Brand:CaymanSKU:11713 - 1 mgAvailable on backorder
Gymnemagenin is the aglycone core of gymnemic acids A and B, triterpenoid sweetness inhibitors derived from G. sylvestre.{39213} It is used as a biomarker for the quantification of gymnemic acids in medicinal plant extracts.{39214}
Brand:CaymanSKU:11713 - 5 mgAvailable on backorder
Gymnemagenin is the aglycone core of gymnemic acids A and B, triterpenoid sweetness inhibitors derived from G. sylvestre.{39213} It is used as a biomarker for the quantification of gymnemic acids in medicinal plant extracts.{39214}
Brand:CaymanSKU:11713 - 500 µgAvailable on backorder
Gymnemic acid I is a triterpene glycoside that has been found in G. sylvestre and has antihyperglycemic activities.{45515,45513} It inhibits glucose-induced phosphorylation of serine 70 on S6 kinase (S6K1) and serine 2448 on mTOR, caspase-3 activity, and apoptosis, as well as increases autophagy in MIN-6 pancreatic β cells when used at a concentration of 5 µg/ml.{45515} Gymnemic acid I has been used as a reference compound to compare the potency of plant-derived sweet taste inhibitors.{45513}
Brand:CaymanSKU:28495 - 1 mgAvailable on backorder
Gymnemic acid I is a triterpene glycoside that has been found in G. sylvestre and has antihyperglycemic activities.{45515,45513} It inhibits glucose-induced phosphorylation of serine 70 on S6 kinase (S6K1) and serine 2448 on mTOR, caspase-3 activity, and apoptosis, as well as increases autophagy in MIN-6 pancreatic β cells when used at a concentration of 5 µg/ml.{45515} Gymnemic acid I has been used as a reference compound to compare the potency of plant-derived sweet taste inhibitors.{45513}
Brand:CaymanSKU:28495 - 5 mgAvailable on backorder
Gymnoascolide A is a fungal metabolite originally isolated from G. reessii that has fungicidal and vasodilatory activities.{45999,55000} It is active against the phytopathogenic fungus S. nodorum (MIC = 13 µg/ml) but not C. albicans, B. subtilis, or the ruminant pathogenic nematode H. contortus in an agar diffusion assay.{45999,55000} Gymnoascolide A (1 µM) inhibits calcium-induced contractions in isolated rat aortic rings.{55000}
Brand:CaymanSKU:28585 - 1 mgAvailable on backorder
Gypenoside IX is a dammarane-type triterpene saponin that has been found in P. notoginseng.{48933} It prevents increases in inducible nitric oxide synthase (iNOS), IL-6, and TNF-α levels, as well as phosphorylation of NF-κB, IκB, p38 MAPK, and Akt, induced by LPS and TNF-α in rat C6 glial cells when used at a concentration of 25 μM.{48934} In vivo, gypenoside IX (30 mg/kg per day) reduces LPS-induced increases in NF-κB, IκB, p38 MAPK, and Akt phosphorylation in mouse brain cortex.
Brand:CaymanSKU:29705 - 10 mgAvailable on backorder
Gypenoside IX is a dammarane-type triterpene saponin that has been found in P. notoginseng.{48933} It prevents increases in inducible nitric oxide synthase (iNOS), IL-6, and TNF-α levels, as well as phosphorylation of NF-κB, IκB, p38 MAPK, and Akt, induced by LPS and TNF-α in rat C6 glial cells when used at a concentration of 25 μM.{48934} In vivo, gypenoside IX (30 mg/kg per day) reduces LPS-induced increases in NF-κB, IκB, p38 MAPK, and Akt phosphorylation in mouse brain cortex.
Brand:CaymanSKU:29705 - 25 mgAvailable on backorder
Gypenoside IX is a dammarane-type triterpene saponin that has been found in P. notoginseng.{48933} It prevents increases in inducible nitric oxide synthase (iNOS), IL-6, and TNF-α levels, as well as phosphorylation of NF-κB, IκB, p38 MAPK, and Akt, induced by LPS and TNF-α in rat C6 glial cells when used at a concentration of 25 μM.{48934} In vivo, gypenoside IX (30 mg/kg per day) reduces LPS-induced increases in NF-κB, IκB, p38 MAPK, and Akt phosphorylation in mouse brain cortex.
Brand:CaymanSKU:29705 - 5 mgAvailable on backorder
Gypenoside IX is a dammarane-type triterpene saponin that has been found in P. notoginseng.{48933} It prevents increases in inducible nitric oxide synthase (iNOS), IL-6, and TNF-α levels, as well as phosphorylation of NF-κB, IκB, p38 MAPK, and Akt, induced by LPS and TNF-α in rat C6 glial cells when used at a concentration of 25 μM.{48934} In vivo, gypenoside IX (30 mg/kg per day) reduces LPS-induced increases in NF-κB, IκB, p38 MAPK, and Akt phosphorylation in mouse brain cortex.
Brand:CaymanSKU:29705 - 50 mgAvailable on backorder
Hydrogen sulfide (H2S) is a gaseous mediator which, like nitric oxide (NO), has numerous profound actions in mammalian physiology. GYY 4137 is a water-soluble, slow-releasing hydrogen sulfide (H2S) donor.{17169} When given intravenously, it demonstrates vasodilator and anti-hypertensive activity in rats, in either the acute (L-NAME-induced) or chronic (spontaneously hypertensive) hypertension models.{17169} Intravenous GYY 4137 also protects against endotoxic shock in rats, inhibiting tumor necrosis factor-α, interleukin (IL)-1β, and IL-6 production and reducing NF-κB activation, iNOS and cyclooxygenase-2 expression, and NO and prostaglandin E2 generation.{17285}
Brand:CaymanSKU:- Hydrogen sulfide (H2S) is a gaseous mediator which, like nitric oxide (NO), has numerous profound actions in mammalian physiology. GYY 4137 is a water-soluble, slow-releasing hydrogen sulfide (H2S) donor.{17169} When given intravenously, it demonstrates vasodilator and anti-hypertensive activity in rats, in either the acute (L-NAME-induced) or chronic (spontaneously hypertensive) hypertension models.{17169} Intravenous GYY 4137 also protects against endotoxic shock in rats, inhibiting tumor necrosis factor-α, interleukin (IL)-1β, and IL-6 production and reducing NF-κB activation, iNOS and cyclooxygenase-2 expression, and NO and prostaglandin E2 generation.{17285}
Brand:CaymanSKU:- Hydrogen sulfide (H2S) is a gaseous mediator which, like nitric oxide (NO), has numerous profound actions in mammalian physiology. GYY 4137 is a water-soluble, slow-releasing hydrogen sulfide (H2S) donor.{17169} When given intravenously, it demonstrates vasodilator and anti-hypertensive activity in rats, in either the acute (L-NAME-induced) or chronic (spontaneously hypertensive) hypertension models.{17169} Intravenous GYY 4137 also protects against endotoxic shock in rats, inhibiting tumor necrosis factor-α, interleukin (IL)-1β, and IL-6 production and reducing NF-κB activation, iNOS and cyclooxygenase-2 expression, and NO and prostaglandin E2 generation.{17285}
Brand:CaymanSKU:- Hydrogen sulfide (H2S) is a gaseous mediator which, like nitric oxide (NO), has numerous profound actions in mammalian physiology. GYY 4137 is a water-soluble, slow-releasing hydrogen sulfide (H2S) donor.{17169} When given intravenously, it demonstrates vasodilator and anti-hypertensive activity in rats, in either the acute (L-NAME-induced) or chronic (spontaneously hypertensive) hypertension models.{17169} Intravenous GYY 4137 also protects against endotoxic shock in rats, inhibiting tumor necrosis factor-α, interleukin (IL)-1β, and IL-6 production and reducing NF-κB activation, iNOS and cyclooxygenase-2 expression, and NO and prostaglandin E2 generation.{17285}
Brand:CaymanSKU:-
GZD-824 is an orally available inhibitor of a broad spectrum of Bcr/Abl tyrosine kinase mutants including T315I (IC50s = 0.34 and 0.68 nM for wild-type Bcr/Abl and Bcr/AblT315I, respectively).{33583} It has been shown to suppress the proliferation of Bcr/Abl-positive K562 and Ku812 human chronic myelogenous leukemia cells (IC50s = 0.2 and 0.13 nM, respectively) and induce tumor regression in mouse xenograft tumor models driven by either wild-type or mutant Bcr/Abl.{33583}
Brand:CaymanSKU:21508 -Out of stock
GZD-824 is an orally available inhibitor of a broad spectrum of Bcr/Abl tyrosine kinase mutants including T315I (IC50s = 0.34 and 0.68 nM for wild-type Bcr/Abl and Bcr/AblT315I, respectively).{33583} It has been shown to suppress the proliferation of Bcr/Abl-positive K562 and Ku812 human chronic myelogenous leukemia cells (IC50s = 0.2 and 0.13 nM, respectively) and induce tumor regression in mouse xenograft tumor models driven by either wild-type or mutant Bcr/Abl.{33583}
Brand:CaymanSKU:21508 -Out of stock
GZD-824 is an orally available inhibitor of a broad spectrum of Bcr/Abl tyrosine kinase mutants including T315I (IC50s = 0.34 and 0.68 nM for wild-type Bcr/Abl and Bcr/AblT315I, respectively).{33583} It has been shown to suppress the proliferation of Bcr/Abl-positive K562 and Ku812 human chronic myelogenous leukemia cells (IC50s = 0.2 and 0.13 nM, respectively) and induce tumor regression in mouse xenograft tumor models driven by either wild-type or mutant Bcr/Abl.{33583}
Brand:CaymanSKU:21508 -Out of stock
GZD-824 is an orally available inhibitor of a broad spectrum of Bcr/Abl tyrosine kinase mutants including T315I (IC50s = 0.34 and 0.68 nM for wild-type Bcr/Abl and Bcr/AblT315I, respectively).{33583} It has been shown to suppress the proliferation of Bcr/Abl-positive K562 and Ku812 human chronic myelogenous leukemia cells (IC50s = 0.2 and 0.13 nM, respectively) and induce tumor regression in mouse xenograft tumor models driven by either wild-type or mutant Bcr/Abl.{33583}
Brand:CaymanSKU:21508 -Out of stock
H-151 is an inhibitor of stimulator of interferon genes (STING).{35390} It forms an adduct with mouse STING in serum and acts in an irreversible manner. It inhibits the type I interferon (IFN) response and reduces the phosphorylation of TBK1 and palmitoylation of human STING (hsSTING) in vitro. It also reduces increases in mouse serum levels of IFN-β and IL-6 induced by the STING agonist 10-carboxymethyl-9-acridanone (CMA).
Brand:CaymanSKU:25857 - 10 mgAvailable on backorder
H-151 is an inhibitor of stimulator of interferon genes (STING).{35390} It forms an adduct with mouse STING in serum and acts in an irreversible manner. It inhibits the type I interferon (IFN) response and reduces the phosphorylation of TBK1 and palmitoylation of human STING (hsSTING) in vitro. It also reduces increases in mouse serum levels of IFN-β and IL-6 induced by the STING agonist 10-carboxymethyl-9-acridanone (CMA).
Brand:CaymanSKU:25857 - 100 mgAvailable on backorder
H-151 is an inhibitor of stimulator of interferon genes (STING).{35390} It forms an adduct with mouse STING in serum and acts in an irreversible manner. It inhibits the type I interferon (IFN) response and reduces the phosphorylation of TBK1 and palmitoylation of human STING (hsSTING) in vitro. It also reduces increases in mouse serum levels of IFN-β and IL-6 induced by the STING agonist 10-carboxymethyl-9-acridanone (CMA).
Brand:CaymanSKU:25857 - 5 mgAvailable on backorder
H-151 is an inhibitor of stimulator of interferon genes (STING).{35390} It forms an adduct with mouse STING in serum and acts in an irreversible manner. It inhibits the type I interferon (IFN) response and reduces the phosphorylation of TBK1 and palmitoylation of human STING (hsSTING) in vitro. It also reduces increases in mouse serum levels of IFN-β and IL-6 induced by the STING agonist 10-carboxymethyl-9-acridanone (CMA).
Brand:CaymanSKU:25857 - 50 mgAvailable on backorder