Chemicals
Showing 21001–21150 of 41137 results
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Golvatinib is an orally bioavailable dual inhibitor of the receptor tyrosine kinases c-Met and VEGF receptor 2 (VEGFR2), which are involved in tumor progression.{41051} Golvatinib inhibits autophosphorylation of c-Met in MKN45 cells and phosphorylation of VEGFR2 in human umbilical vein endothelial cells (HUVECs; IC50s = 14 and 16 nM, respectively). It also inhibits proliferation of a variety of cancer cell lines and of HUVECs stimulated with hepatocyte growth factor (HGF) and VEGF but not bFGF (IC50s = 17, 84, and >1,000 nM for HGF-, VEGF-, and bFGF-stimulated HUVECs, respectively). In nude mouse xenograft models using MKN45, Hs746T, SNU-5, or EBC-1 cancer cells, golvatinib (25-200 mg/kg, daily) dose-dependently reduces tumor volume, and it increases survival in the model using MKN45 cells.
Brand:CaymanSKU:22143 -Out of stock
Gomisin C, a lignan first isolated from the fruits of S. chinensis, scavenges oxygen radicals and reduces the production of reactive oxygen species by inhibiting neutrophil activity.{30125} It has been shown to attenuate respiratory burst in rat peripheral neutrophils via suppression of NADPH oxidase (39% inhibition at 30 µg/ml) and inhibition of cytosolic calcium release from intracellular stores (36% inhibition at 50 µg/ml).{30126} Gomisin C can induce liver microsomal cytochrome P450, thus facilitating the clearance of xenobiotics and protecting against hepatotoxicity in rodent models of liver injury.{30124}
Brand:CaymanSKU:-Available on backorder
Gomisin C, a lignan first isolated from the fruits of S. chinensis, scavenges oxygen radicals and reduces the production of reactive oxygen species by inhibiting neutrophil activity.{30125} It has been shown to attenuate respiratory burst in rat peripheral neutrophils via suppression of NADPH oxidase (39% inhibition at 30 µg/ml) and inhibition of cytosolic calcium release from intracellular stores (36% inhibition at 50 µg/ml).{30126} Gomisin C can induce liver microsomal cytochrome P450, thus facilitating the clearance of xenobiotics and protecting against hepatotoxicity in rodent models of liver injury.{30124}
Brand:CaymanSKU:-Available on backorder
Gomisin C, a lignan first isolated from the fruits of S. chinensis, scavenges oxygen radicals and reduces the production of reactive oxygen species by inhibiting neutrophil activity.{30125} It has been shown to attenuate respiratory burst in rat peripheral neutrophils via suppression of NADPH oxidase (39% inhibition at 30 µg/ml) and inhibition of cytosolic calcium release from intracellular stores (36% inhibition at 50 µg/ml).{30126} Gomisin C can induce liver microsomal cytochrome P450, thus facilitating the clearance of xenobiotics and protecting against hepatotoxicity in rodent models of liver injury.{30124}
Brand:CaymanSKU:-Available on backorder
Gomisin C, a lignan first isolated from the fruits of S. chinensis, scavenges oxygen radicals and reduces the production of reactive oxygen species by inhibiting neutrophil activity.{30125} It has been shown to attenuate respiratory burst in rat peripheral neutrophils via suppression of NADPH oxidase (39% inhibition at 30 µg/ml) and inhibition of cytosolic calcium release from intracellular stores (36% inhibition at 50 µg/ml).{30126} Gomisin C can induce liver microsomal cytochrome P450, thus facilitating the clearance of xenobiotics and protecting against hepatotoxicity in rodent models of liver injury.{30124}
Brand:CaymanSKU:-Available on backorder
Gomisin D is a lignan that has been found in S. chinensis and has diverse biological activities, including enzyme inhibitory and antioxidant properties.{52842,52843,47352} It inhibits acetylcholinesterase (AChE) with an IC50 value of 7.84 µM.{52842} Gomisin D scavenges ABTS (Item No. 27317) and 2,2-diphenyl-1-picrylhydrazyl (DPPH; Item No. 14805) radicals (IC50s = 24.5 and 203 µM, respectively).{47352} It inhibits the UDP-glucuronosyltransferase (UGT) isoforms UGT1A1 and UGT1A3 by 89.9 and 83.1%, respectively, when used at a concentration of 100 µM.{52843} It is selective for UGT1A1 and UGT1A3 over other UGT isoforms at 100 µM.
Brand:CaymanSKU:30697 - 1 mgAvailable on backorder
Gomisin D is a lignan that has been found in S. chinensis and has diverse biological activities, including enzyme inhibitory and antioxidant properties.{52842,52843,47352} It inhibits acetylcholinesterase (AChE) with an IC50 value of 7.84 µM.{52842} Gomisin D scavenges ABTS (Item No. 27317) and 2,2-diphenyl-1-picrylhydrazyl (DPPH; Item No. 14805) radicals (IC50s = 24.5 and 203 µM, respectively).{47352} It inhibits the UDP-glucuronosyltransferase (UGT) isoforms UGT1A1 and UGT1A3 by 89.9 and 83.1%, respectively, when used at a concentration of 100 µM.{52843} It is selective for UGT1A1 and UGT1A3 over other UGT isoforms at 100 µM.
Brand:CaymanSKU:30697 - 10 mgAvailable on backorder
Gomisin D is a lignan that has been found in S. chinensis and has diverse biological activities, including enzyme inhibitory and antioxidant properties.{52842,52843,47352} It inhibits acetylcholinesterase (AChE) with an IC50 value of 7.84 µM.{52842} Gomisin D scavenges ABTS (Item No. 27317) and 2,2-diphenyl-1-picrylhydrazyl (DPPH; Item No. 14805) radicals (IC50s = 24.5 and 203 µM, respectively).{47352} It inhibits the UDP-glucuronosyltransferase (UGT) isoforms UGT1A1 and UGT1A3 by 89.9 and 83.1%, respectively, when used at a concentration of 100 µM.{52843} It is selective for UGT1A1 and UGT1A3 over other UGT isoforms at 100 µM.
Brand:CaymanSKU:30697 - 5 mgAvailable on backorder
Gomisin J is a lignan that has been found in Schisandra chinensis and has diverse biological activities.{52505,52506} It inhibits HIV-1 IIIB replication in H9 T cells (EC50 = 1.5 µg/ml).{52505} Gomisin J (20 µM) decreases LPS-induced increases in nitric oxide (NO) production and p38, ERK, and JNK phosphorylation in RAW 264.7 cells.{52506} It induces relaxation of isolated, precontracted endothelium-intact rat aortic rings when used at concentrations of 3, 10, and 30 µg/ml.{52508} Gomisin J is cytotoxic to 13 cancer cell lines, including breast, colon, and cervical cancer cells, when used at a concentration of 30 µg/ml.{52507}
Brand:CaymanSKU:30213 - 1 mgAvailable on backorder
Gomisin J is a lignan that has been found in Schisandra chinensis and has diverse biological activities.{52505,52506} It inhibits HIV-1 IIIB replication in H9 T cells (EC50 = 1.5 µg/ml).{52505} Gomisin J (20 µM) decreases LPS-induced increases in nitric oxide (NO) production and p38, ERK, and JNK phosphorylation in RAW 264.7 cells.{52506} It induces relaxation of isolated, precontracted endothelium-intact rat aortic rings when used at concentrations of 3, 10, and 30 µg/ml.{52508} Gomisin J is cytotoxic to 13 cancer cell lines, including breast, colon, and cervical cancer cells, when used at a concentration of 30 µg/ml.{52507}
Brand:CaymanSKU:30213 - 10 mgAvailable on backorder
Gomisin J is a lignan that has been found in Schisandra chinensis and has diverse biological activities.{52505,52506} It inhibits HIV-1 IIIB replication in H9 T cells (EC50 = 1.5 µg/ml).{52505} Gomisin J (20 µM) decreases LPS-induced increases in nitric oxide (NO) production and p38, ERK, and JNK phosphorylation in RAW 264.7 cells.{52506} It induces relaxation of isolated, precontracted endothelium-intact rat aortic rings when used at concentrations of 3, 10, and 30 µg/ml.{52508} Gomisin J is cytotoxic to 13 cancer cell lines, including breast, colon, and cervical cancer cells, when used at a concentration of 30 µg/ml.{52507}
Brand:CaymanSKU:30213 - 5 mgAvailable on backorder
Gonadorelin is a tropic hormone and agonist of the gonadotropin-releasing hormone receptor (GNRHR; Ki = 13 nM in CHO cells expressing the human receptor).{36464} It stimulates luteinizing hormone (LH) and follicle-stimulating hormone (FSH) release from rat anterior pituitary cultures when administered at a dose of 0.1 μg.{40777} It also stimulates LH release from bovine anterior pituitary cultures at a concentration of 1 μM.{40778} In vivo, gonadorelin induces ovulation in rats pretreated with fluphenazine (Item No. 23555; ED50 = 610.3 ng/kg).{40779} Formulations containing gonadorelin have been used as diagnostic agents to assess pituitary gland function.
Brand:CaymanSKU:24240 - 10 mgAvailable on backorder
Gonadorelin is a tropic hormone and agonist of the gonadotropin-releasing hormone receptor (GNRHR; Ki = 13 nM in CHO cells expressing the human receptor).{36464} It stimulates luteinizing hormone (LH) and follicle-stimulating hormone (FSH) release from rat anterior pituitary cultures when administered at a dose of 0.1 μg.{40777} It also stimulates LH release from bovine anterior pituitary cultures at a concentration of 1 μM.{40778} In vivo, gonadorelin induces ovulation in rats pretreated with fluphenazine (Item No. 23555; ED50 = 610.3 ng/kg).{40779} Formulations containing gonadorelin have been used as diagnostic agents to assess pituitary gland function.
Brand:CaymanSKU:24240 - 25 mgAvailable on backorder
Gonadorelin is a tropic hormone and agonist of the gonadotropin-releasing hormone receptor (GNRHR; Ki = 13 nM in CHO cells expressing the human receptor).{36464} It stimulates luteinizing hormone (LH) and follicle-stimulating hormone (FSH) release from rat anterior pituitary cultures when administered at a dose of 0.1 μg.{40777} It also stimulates LH release from bovine anterior pituitary cultures at a concentration of 1 μM.{40778} In vivo, gonadorelin induces ovulation in rats pretreated with fluphenazine (Item No. 23555; ED50 = 610.3 ng/kg).{40779} Formulations containing gonadorelin have been used as diagnostic agents to assess pituitary gland function.
Brand:CaymanSKU:24240 - 5 mgAvailable on backorder
Goserelin is a synthetic gonadotropin-releasing hormone (GNRH) agonist that binds to the GNRH receptor (GNRHR; Ki = 1.6 nM, in CHO cells expressing the human receptor).{36464} It binds to mouse pituitary αT3-1 cells and human placenta (Kds = 2 and 580 nM, respectively) and increases intracellular calcium in αT3-1 cells.{36465} Goserelin induces testosterone production in vitro within 4 h in rat Leydig cells (ED50 = 83 nM) but decreases testosterone plasma level in vivo in rats over a period of 2 to 24 weeks.{36466,36467} It inhibits tumor growth in a DU145 human prostate carcinoma mouse xenograft model when administered at a dose of 100 μg per day.{36468} Formulations containing goserelin have been used in the treatment of hormone-dependent breast and prostate cancers, as well as endometriosis and uterine fibroids.
Brand:CaymanSKU:24071 - 1 mgAvailable on backorder
Goserelin is a synthetic gonadotropin-releasing hormone (GNRH) agonist that binds to the GNRH receptor (GNRHR; Ki = 1.6 nM, in CHO cells expressing the human receptor).{36464} It binds to mouse pituitary αT3-1 cells and human placenta (Kds = 2 and 580 nM, respectively) and increases intracellular calcium in αT3-1 cells.{36465} Goserelin induces testosterone production in vitro within 4 h in rat Leydig cells (ED50 = 83 nM) but decreases testosterone plasma level in vivo in rats over a period of 2 to 24 weeks.{36466,36467} It inhibits tumor growth in a DU145 human prostate carcinoma mouse xenograft model when administered at a dose of 100 μg per day.{36468} Formulations containing goserelin have been used in the treatment of hormone-dependent breast and prostate cancers, as well as endometriosis and uterine fibroids.
Brand:CaymanSKU:24071 - 10 mgAvailable on backorder
Goserelin is a synthetic gonadotropin-releasing hormone (GNRH) agonist that binds to the GNRH receptor (GNRHR; Ki = 1.6 nM, in CHO cells expressing the human receptor).{36464} It binds to mouse pituitary αT3-1 cells and human placenta (Kds = 2 and 580 nM, respectively) and increases intracellular calcium in αT3-1 cells.{36465} Goserelin induces testosterone production in vitro within 4 h in rat Leydig cells (ED50 = 83 nM) but decreases testosterone plasma level in vivo in rats over a period of 2 to 24 weeks.{36466,36467} It inhibits tumor growth in a DU145 human prostate carcinoma mouse xenograft model when administered at a dose of 100 μg per day.{36468} Formulations containing goserelin have been used in the treatment of hormone-dependent breast and prostate cancers, as well as endometriosis and uterine fibroids.
Brand:CaymanSKU:24071 - 5 mgAvailable on backorder
Gossypol is a racemic mixture of natural polyphenols isolated from parts of the cotton plant (genus Gossypium). It causes infertility in a variety of cotton pests and spermatogenesis arrest in humans.{23003} Gossypol also has antimalarial properties, preventing the growth of P. falciparum at low micromolar concentrations.{23001} It inhibits aldose reductase (Ki = 0.5 µM).{23002} Gossypol also acts as an anticancer agent, inhibiting cell growth in various cancer cell lines, in part by blocking the anti-apoptotic functions of Bcl-2 and Bcl-xL, again at low micromolar concentrations.{23000}
Brand:CaymanSKU:-Gossypol is a racemic mixture of natural polyphenols isolated from parts of the cotton plant (genus Gossypium). It causes infertility in a variety of cotton pests and spermatogenesis arrest in humans.{23003} Gossypol also has antimalarial properties, preventing the growth of P. falciparum at low micromolar concentrations.{23001} It inhibits aldose reductase (Ki = 0.5 µM).{23002} Gossypol also acts as an anticancer agent, inhibiting cell growth in various cancer cell lines, in part by blocking the anti-apoptotic functions of Bcl-2 and Bcl-xL, again at low micromolar concentrations.{23000}
Brand:CaymanSKU:-Gossypol is a racemic mixture of natural polyphenols isolated from parts of the cotton plant (genus Gossypium). It causes infertility in a variety of cotton pests and spermatogenesis arrest in humans.{23003} Gossypol also has antimalarial properties, preventing the growth of P. falciparum at low micromolar concentrations.{23001} It inhibits aldose reductase (Ki = 0.5 µM).{23002} Gossypol also acts as an anticancer agent, inhibiting cell growth in various cancer cell lines, in part by blocking the anti-apoptotic functions of Bcl-2 and Bcl-xL, again at low micromolar concentrations.{23000}
Brand:CaymanSKU:-Gossypol is a racemic mixture of natural polyphenols isolated from parts of the cotton plant (genus Gossypium). It causes infertility in a variety of cotton pests and spermatogenesis arrest in humans.{23003} Gossypol also has antimalarial properties, preventing the growth of P. falciparum at low micromolar concentrations.{23001} It inhibits aldose reductase (Ki = 0.5 µM).{23002} Gossypol also acts as an anticancer agent, inhibiting cell growth in various cancer cell lines, in part by blocking the anti-apoptotic functions of Bcl-2 and Bcl-xL, again at low micromolar concentrations.{23000}
Brand:CaymanSKU:-Nicotinamide phosphoribosyltransferase (Nampt) converts nicotinamide into nicotinamide mononucleotide (NMN), which is subsequently converted to NAD+ by NMN adenyltransferase. Cancer cells commonly have an unusually high rate of NAD+ turnover, suggesting that inhibition of Nampt might selectively target cancer cells. GPP 78 is a potent inhibitor of Nampt (IC50 = 3 nM).{17893} It induces cell death in the neuroblastoma cell line SH-SY5Y with an IC50 value of 3.8 nM through a process that appears to involve autophagy.{13670}
Brand:CaymanSKU:-Nicotinamide phosphoribosyltransferase (Nampt) converts nicotinamide into nicotinamide mononucleotide (NMN), which is subsequently converted to NAD+ by NMN adenyltransferase. Cancer cells commonly have an unusually high rate of NAD+ turnover, suggesting that inhibition of Nampt might selectively target cancer cells. GPP 78 is a potent inhibitor of Nampt (IC50 = 3 nM).{17893} It induces cell death in the neuroblastoma cell line SH-SY5Y with an IC50 value of 3.8 nM through a process that appears to involve autophagy.{13670}
Brand:CaymanSKU:-Nicotinamide phosphoribosyltransferase (Nampt) converts nicotinamide into nicotinamide mononucleotide (NMN), which is subsequently converted to NAD+ by NMN adenyltransferase. Cancer cells commonly have an unusually high rate of NAD+ turnover, suggesting that inhibition of Nampt might selectively target cancer cells. GPP 78 is a potent inhibitor of Nampt (IC50 = 3 nM).{17893} It induces cell death in the neuroblastoma cell line SH-SY5Y with an IC50 value of 3.8 nM through a process that appears to involve autophagy.{13670}
Brand:CaymanSKU:-Nicotinamide phosphoribosyltransferase (Nampt) converts nicotinamide into nicotinamide mononucleotide (NMN), which is subsequently converted to NAD+ by NMN adenyltransferase. Cancer cells commonly have an unusually high rate of NAD+ turnover, suggesting that inhibition of Nampt might selectively target cancer cells. GPP 78 is a potent inhibitor of Nampt (IC50 = 3 nM).{17893} It induces cell death in the neuroblastoma cell line SH-SY5Y with an IC50 value of 3.8 nM through a process that appears to involve autophagy.{13670}
Brand:CaymanSKU:-GPR120 (free fatty acid receptor 4/FFAR4) is a G protein-coupled receptor expressed in intestine, adipocytes, and pro-inflammatory macrophages that is activated by long chain free fatty acids. It has been linked to the ability of fatty acids to produce anti-inflammatory effects and to acutely potentiate insulin secretion. GPR120 compound A is an orally available, high-affinity agonist of GPR120 (EC50 = ~0.35 µM) that demonstrates potent selectivity over another lipid-sensing G-protein, GPR40 (FFAR1).{26948} This compound exerts anti-inflammatory effects on macrophages in vitro and improves glucose tolerance, decreases hyperinsulinemia, increases insulin sensitivity, and decreases hepatic steatosis when included at 30 mg/kg body weight in a high-fat diet fed to obese mice.{26948}
Brand:CaymanSKU:-Out of stock
GPR120 (free fatty acid receptor 4/FFAR4) is a G protein-coupled receptor expressed in intestine, adipocytes, and pro-inflammatory macrophages that is activated by long chain free fatty acids. It has been linked to the ability of fatty acids to produce anti-inflammatory effects and to acutely potentiate insulin secretion. GPR120 compound A is an orally available, high-affinity agonist of GPR120 (EC50 = ~0.35 µM) that demonstrates potent selectivity over another lipid-sensing G-protein, GPR40 (FFAR1).{26948} This compound exerts anti-inflammatory effects on macrophages in vitro and improves glucose tolerance, decreases hyperinsulinemia, increases insulin sensitivity, and decreases hepatic steatosis when included at 30 mg/kg body weight in a high-fat diet fed to obese mice.{26948}
Brand:CaymanSKU:-Out of stock
GPR120 (free fatty acid receptor 4/FFAR4) is a G protein-coupled receptor expressed in intestine, adipocytes, and pro-inflammatory macrophages that is activated by long chain free fatty acids. It has been linked to the ability of fatty acids to produce anti-inflammatory effects and to acutely potentiate insulin secretion. GPR120 compound A is an orally available, high-affinity agonist of GPR120 (EC50 = ~0.35 µM) that demonstrates potent selectivity over another lipid-sensing G-protein, GPR40 (FFAR1).{26948} This compound exerts anti-inflammatory effects on macrophages in vitro and improves glucose tolerance, decreases hyperinsulinemia, increases insulin sensitivity, and decreases hepatic steatosis when included at 30 mg/kg body weight in a high-fat diet fed to obese mice.{26948}
Brand:CaymanSKU:-Out of stock
GPR120 (free fatty acid receptor 4/FFAR4) is a G protein-coupled receptor expressed in intestine, adipocytes, and pro-inflammatory macrophages that is activated by long chain free fatty acids. It has been linked to the ability of fatty acids to produce anti-inflammatory effects and to acutely potentiate insulin secretion. GPR120 compound A is an orally available, high-affinity agonist of GPR120 (EC50 = ~0.35 µM) that demonstrates potent selectivity over another lipid-sensing G-protein, GPR40 (FFAR1).{26948} This compound exerts anti-inflammatory effects on macrophages in vitro and improves glucose tolerance, decreases hyperinsulinemia, increases insulin sensitivity, and decreases hepatic steatosis when included at 30 mg/kg body weight in a high-fat diet fed to obese mice.{26948}
Brand:CaymanSKU:-Out of stock
GPR39-C3 is a potent agonist of the orphan G protein-coupled receptor GPR39 with EC50 values of 0.8 and 0.4 nM for cAMP production in HEK293 cells expressing human and rat receptors, respectively.{42282} It is selective for GPR39 over a panel of kinases (IC50s = >10 μM), ghrelin and neurotensin-1 receptors (IC50s = >30 μM), and a variety of enzymes, transporters, or G protein-coupled receptors. GPR39-C3 increases secretion of glucagon-like peptide 1 (GLP-1; Item No. 24460) in STC-1 mouse enteroendocrine cells (EC50 = 0.06 μM) and is protective against cytokine-induced cell death in INS-1E rat insulinoma cells (EC50 = 0.02 μM). In vivo, GPR39-C3 (30 mg/kg) increases the amount of active GLP-1 in sera by 6-fold in glucose-challenged mice when administered concurrently with a dipeptidyl peptidase 4 (DPP-4) inhibitor.
Brand:CaymanSKU:25445 - 1 mgAvailable on backorder
GPR39-C3 is a potent agonist of the orphan G protein-coupled receptor GPR39 with EC50 values of 0.8 and 0.4 nM for cAMP production in HEK293 cells expressing human and rat receptors, respectively.{42282} It is selective for GPR39 over a panel of kinases (IC50s = >10 μM), ghrelin and neurotensin-1 receptors (IC50s = >30 μM), and a variety of enzymes, transporters, or G protein-coupled receptors. GPR39-C3 increases secretion of glucagon-like peptide 1 (GLP-1; Item No. 24460) in STC-1 mouse enteroendocrine cells (EC50 = 0.06 μM) and is protective against cytokine-induced cell death in INS-1E rat insulinoma cells (EC50 = 0.02 μM). In vivo, GPR39-C3 (30 mg/kg) increases the amount of active GLP-1 in sera by 6-fold in glucose-challenged mice when administered concurrently with a dipeptidyl peptidase 4 (DPP-4) inhibitor.
Brand:CaymanSKU:25445 - 10 mgAvailable on backorder
GPR39-C3 is a potent agonist of the orphan G protein-coupled receptor GPR39 with EC50 values of 0.8 and 0.4 nM for cAMP production in HEK293 cells expressing human and rat receptors, respectively.{42282} It is selective for GPR39 over a panel of kinases (IC50s = >10 μM), ghrelin and neurotensin-1 receptors (IC50s = >30 μM), and a variety of enzymes, transporters, or G protein-coupled receptors. GPR39-C3 increases secretion of glucagon-like peptide 1 (GLP-1; Item No. 24460) in STC-1 mouse enteroendocrine cells (EC50 = 0.06 μM) and is protective against cytokine-induced cell death in INS-1E rat insulinoma cells (EC50 = 0.02 μM). In vivo, GPR39-C3 (30 mg/kg) increases the amount of active GLP-1 in sera by 6-fold in glucose-challenged mice when administered concurrently with a dipeptidyl peptidase 4 (DPP-4) inhibitor.
Brand:CaymanSKU:25445 - 25 mgAvailable on backorder
GPR39-C3 is a potent agonist of the orphan G protein-coupled receptor GPR39 with EC50 values of 0.8 and 0.4 nM for cAMP production in HEK293 cells expressing human and rat receptors, respectively.{42282} It is selective for GPR39 over a panel of kinases (IC50s = >10 μM), ghrelin and neurotensin-1 receptors (IC50s = >30 μM), and a variety of enzymes, transporters, or G protein-coupled receptors. GPR39-C3 increases secretion of glucagon-like peptide 1 (GLP-1; Item No. 24460) in STC-1 mouse enteroendocrine cells (EC50 = 0.06 μM) and is protective against cytokine-induced cell death in INS-1E rat insulinoma cells (EC50 = 0.02 μM). In vivo, GPR39-C3 (30 mg/kg) increases the amount of active GLP-1 in sera by 6-fold in glucose-challenged mice when administered concurrently with a dipeptidyl peptidase 4 (DPP-4) inhibitor.
Brand:CaymanSKU:25445 - 5 mgAvailable on backorder
Full activation of peroxisome proliferator-activated receptor γ (PPARγ), e.g., using thiazolidinediones, effectively treats insulin resistance and type 2 diabetes but also commonly promotes weight gain, hyperphagia, and edema.{21030} GQ-16 is a partial agonist for PPARγ (Ki = 160 nM) which induces adipogenesis significantly less than the full activator rosiglitazone.{21030} Like rosiglitazone, GQ-16 reverses high fat diet-mediated impairments in insulin signaling.{21030} However, GQ-16 does not induce weight gain, hyperphagia, or edema. GQ-16 does not activate PPARα, PPARβ/δ, or RXRα.{21030}
Brand:CaymanSKU:11908 - 10 mgAvailable on backorder
Full activation of peroxisome proliferator-activated receptor γ (PPARγ), e.g., using thiazolidinediones, effectively treats insulin resistance and type 2 diabetes but also commonly promotes weight gain, hyperphagia, and edema.{21030} GQ-16 is a partial agonist for PPARγ (Ki = 160 nM) which induces adipogenesis significantly less than the full activator rosiglitazone.{21030} Like rosiglitazone, GQ-16 reverses high fat diet-mediated impairments in insulin signaling.{21030} However, GQ-16 does not induce weight gain, hyperphagia, or edema. GQ-16 does not activate PPARα, PPARβ/δ, or RXRα.{21030}
Brand:CaymanSKU:11908 - 100 mgAvailable on backorder
Full activation of peroxisome proliferator-activated receptor γ (PPARγ), e.g., using thiazolidinediones, effectively treats insulin resistance and type 2 diabetes but also commonly promotes weight gain, hyperphagia, and edema.{21030} GQ-16 is a partial agonist for PPARγ (Ki = 160 nM) which induces adipogenesis significantly less than the full activator rosiglitazone.{21030} Like rosiglitazone, GQ-16 reverses high fat diet-mediated impairments in insulin signaling.{21030} However, GQ-16 does not induce weight gain, hyperphagia, or edema. GQ-16 does not activate PPARα, PPARβ/δ, or RXRα.{21030}
Brand:CaymanSKU:11908 - 5 mgAvailable on backorder
Full activation of peroxisome proliferator-activated receptor γ (PPARγ), e.g., using thiazolidinediones, effectively treats insulin resistance and type 2 diabetes but also commonly promotes weight gain, hyperphagia, and edema.{21030} GQ-16 is a partial agonist for PPARγ (Ki = 160 nM) which induces adipogenesis significantly less than the full activator rosiglitazone.{21030} Like rosiglitazone, GQ-16 reverses high fat diet-mediated impairments in insulin signaling.{21030} However, GQ-16 does not induce weight gain, hyperphagia, or edema. GQ-16 does not activate PPARα, PPARβ/δ, or RXRα.{21030}
Brand:CaymanSKU:11908 - 50 mgAvailable on backorder
GR113808 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT4.{42967} It binds to 5-HT4 receptors with an IC50 value of 0.4 nM in COS-7 cells expressing the human recombinant receptor and in guinea pig striatal membranes (IC50 = 0.5 nM).{42968} GR113808 is selective for 5-HT4 receptors over 5-HT1 receptors (Kis = >10 µM in dog saphenous vein and porcine vena cava), as well as 5-HT2 and 5-HT3 receptors (Kis = >10 and 1 μM in rabbit thoracic aorta and rat cerebral cortex, respectively).{42967} It is also selective for 5-HT4 over adenosine, adrenergic, dopamine, GABA, muscarinic, nicotinic, histamine, and NMDA receptors (Kis = >10 μM for all). GR113808 inhibits relaxation induced by 5-HT (Item No. 14332) in rat thoracic esophagus precontracted by carbachol (carbamoylcholine; Item No. 14486; pA2 = 9.3). In vivo, GR113808 inhibits 5-methoxytryptamine-induced tachycardia in anaesthetized piglets.
Brand:CaymanSKU:28733 - 10 mgAvailable on backorder
GR113808 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT4.{42967} It binds to 5-HT4 receptors with an IC50 value of 0.4 nM in COS-7 cells expressing the human recombinant receptor and in guinea pig striatal membranes (IC50 = 0.5 nM).{42968} GR113808 is selective for 5-HT4 receptors over 5-HT1 receptors (Kis = >10 µM in dog saphenous vein and porcine vena cava), as well as 5-HT2 and 5-HT3 receptors (Kis = >10 and 1 μM in rabbit thoracic aorta and rat cerebral cortex, respectively).{42967} It is also selective for 5-HT4 over adenosine, adrenergic, dopamine, GABA, muscarinic, nicotinic, histamine, and NMDA receptors (Kis = >10 μM for all). GR113808 inhibits relaxation induced by 5-HT (Item No. 14332) in rat thoracic esophagus precontracted by carbachol (carbamoylcholine; Item No. 14486; pA2 = 9.3). In vivo, GR113808 inhibits 5-methoxytryptamine-induced tachycardia in anaesthetized piglets.
Brand:CaymanSKU:28733 - 25 mgAvailable on backorder
GR113808 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT4.{42967} It binds to 5-HT4 receptors with an IC50 value of 0.4 nM in COS-7 cells expressing the human recombinant receptor and in guinea pig striatal membranes (IC50 = 0.5 nM).{42968} GR113808 is selective for 5-HT4 receptors over 5-HT1 receptors (Kis = >10 µM in dog saphenous vein and porcine vena cava), as well as 5-HT2 and 5-HT3 receptors (Kis = >10 and 1 μM in rabbit thoracic aorta and rat cerebral cortex, respectively).{42967} It is also selective for 5-HT4 over adenosine, adrenergic, dopamine, GABA, muscarinic, nicotinic, histamine, and NMDA receptors (Kis = >10 μM for all). GR113808 inhibits relaxation induced by 5-HT (Item No. 14332) in rat thoracic esophagus precontracted by carbachol (carbamoylcholine; Item No. 14486; pA2 = 9.3). In vivo, GR113808 inhibits 5-methoxytryptamine-induced tachycardia in anaesthetized piglets.
Brand:CaymanSKU:28733 - 5 mgAvailable on backorder
GR113808 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT4.{42967} It binds to 5-HT4 receptors with an IC50 value of 0.4 nM in COS-7 cells expressing the human recombinant receptor and in guinea pig striatal membranes (IC50 = 0.5 nM).{42968} GR113808 is selective for 5-HT4 receptors over 5-HT1 receptors (Kis = >10 µM in dog saphenous vein and porcine vena cava), as well as 5-HT2 and 5-HT3 receptors (Kis = >10 and 1 μM in rabbit thoracic aorta and rat cerebral cortex, respectively).{42967} It is also selective for 5-HT4 over adenosine, adrenergic, dopamine, GABA, muscarinic, nicotinic, histamine, and NMDA receptors (Kis = >10 μM for all). GR113808 inhibits relaxation induced by 5-HT (Item No. 14332) in rat thoracic esophagus precontracted by carbachol (carbamoylcholine; Item No. 14486; pA2 = 9.3). In vivo, GR113808 inhibits 5-methoxytryptamine-induced tachycardia in anaesthetized piglets.
Brand:CaymanSKU:28733 - 50 mgAvailable on backorder
GR127935 is an antagonist of the serotonin (5-HT) receptor subtypes 5-HT1B, 5-HT1Dα, and 5-HT1Dβ (IC50s = 3.16, 1.26, and 0.13 nM, respectively).{53337} It is selective for the 5-HT1B and 5-HT1D receptors over other 5-HT receptors (IC50s = 39.81->10,000 nM in radioligand binding assays). GR127935 increases extracellular 5-HT levels in the guinea pig frontal cortex and prevents increases in 5-HT in rat frontal cortex induced by the selective serotonin reuptake inhibitor paroxetine (Item No. 14998).{53338} It enhances memory consolidation in an autoshaping learning task in rats when administered post-training at a dose of 10 mg/kg.{53339} It has been used to elucidate the 5-HT receptor subtypes involved in the anti-inflammatory activity of sumatriptan (Item No. 14600) following myocardial ischemia-reperfusion injury and testicular torsion/detorsion.{53340,53341}
Brand:CaymanSKU:29651 - 10 mgAvailable on backorder
GR127935 is an antagonist of the serotonin (5-HT) receptor subtypes 5-HT1B, 5-HT1Dα, and 5-HT1Dβ (IC50s = 3.16, 1.26, and 0.13 nM, respectively).{53337} It is selective for the 5-HT1B and 5-HT1D receptors over other 5-HT receptors (IC50s = 39.81->10,000 nM in radioligand binding assays). GR127935 increases extracellular 5-HT levels in the guinea pig frontal cortex and prevents increases in 5-HT in rat frontal cortex induced by the selective serotonin reuptake inhibitor paroxetine (Item No. 14998).{53338} It enhances memory consolidation in an autoshaping learning task in rats when administered post-training at a dose of 10 mg/kg.{53339} It has been used to elucidate the 5-HT receptor subtypes involved in the anti-inflammatory activity of sumatriptan (Item No. 14600) following myocardial ischemia-reperfusion injury and testicular torsion/detorsion.{53340,53341}
Brand:CaymanSKU:29651 - 25 mgAvailable on backorder
GR127935 is an antagonist of the serotonin (5-HT) receptor subtypes 5-HT1B, 5-HT1Dα, and 5-HT1Dβ (IC50s = 3.16, 1.26, and 0.13 nM, respectively).{53337} It is selective for the 5-HT1B and 5-HT1D receptors over other 5-HT receptors (IC50s = 39.81->10,000 nM in radioligand binding assays). GR127935 increases extracellular 5-HT levels in the guinea pig frontal cortex and prevents increases in 5-HT in rat frontal cortex induced by the selective serotonin reuptake inhibitor paroxetine (Item No. 14998).{53338} It enhances memory consolidation in an autoshaping learning task in rats when administered post-training at a dose of 10 mg/kg.{53339} It has been used to elucidate the 5-HT receptor subtypes involved in the anti-inflammatory activity of sumatriptan (Item No. 14600) following myocardial ischemia-reperfusion injury and testicular torsion/detorsion.{53340,53341}
Brand:CaymanSKU:29651 - 5 mgAvailable on backorder
GR127935 is an antagonist of the serotonin (5-HT) receptor subtypes 5-HT1B, 5-HT1Dα, and 5-HT1Dβ (IC50s = 3.16, 1.26, and 0.13 nM, respectively).{53337} It is selective for the 5-HT1B and 5-HT1D receptors over other 5-HT receptors (IC50s = 39.81->10,000 nM in radioligand binding assays). GR127935 increases extracellular 5-HT levels in the guinea pig frontal cortex and prevents increases in 5-HT in rat frontal cortex induced by the selective serotonin reuptake inhibitor paroxetine (Item No. 14998).{53338} It enhances memory consolidation in an autoshaping learning task in rats when administered post-training at a dose of 10 mg/kg.{53339} It has been used to elucidate the 5-HT receptor subtypes involved in the anti-inflammatory activity of sumatriptan (Item No. 14600) following myocardial ischemia-reperfusion injury and testicular torsion/detorsion.{53340,53341}
Brand:CaymanSKU:29651 - 50 mgAvailable on backorder
GR148672X is an inhibitor of triacylglycerol hydrolase/carboxylesterase 1 (TGH/CES1; IC50 = 4 nM for the human hepatic enzyme).{45656,45657} It is selective for TGH/CES1 over lipoprotein lipase (LPL) at 5 μM.{45656} GR148672X (25 mg/kg twice per day) decreases plasma levels of triglycerides, total, VLDL, and LDL cholesterol, and apolipoprotein B-100 (ApoB-100) in hamsters.
Brand:CaymanSKU:28756 - 1 mgAvailable on backorder
GR148672X is an inhibitor of triacylglycerol hydrolase/carboxylesterase 1 (TGH/CES1; IC50 = 4 nM for the human hepatic enzyme).{45656,45657} It is selective for TGH/CES1 over lipoprotein lipase (LPL) at 5 μM.{45656} GR148672X (25 mg/kg twice per day) decreases plasma levels of triglycerides, total, VLDL, and LDL cholesterol, and apolipoprotein B-100 (ApoB-100) in hamsters.
Brand:CaymanSKU:28756 - 10 mgAvailable on backorder
GR148672X is an inhibitor of triacylglycerol hydrolase/carboxylesterase 1 (TGH/CES1; IC50 = 4 nM for the human hepatic enzyme).{45656,45657} It is selective for TGH/CES1 over lipoprotein lipase (LPL) at 5 μM.{45656} GR148672X (25 mg/kg twice per day) decreases plasma levels of triglycerides, total, VLDL, and LDL cholesterol, and apolipoprotein B-100 (ApoB-100) in hamsters.
Brand:CaymanSKU:28756 - 5 mgAvailable on backorder
GR159897 is a nonpeptide antagonist of the neurokinin-2 (NK2) receptor.{60141} It binds to NK2 receptors (Ki = 0.32 nM) and is selective for NK2 over NK1 and NK3 receptors in radioligand binding assays (Kis = 5,010 and >1,000 nM, respectively). GR159897 inhibits contractions induced by the NK2 receptor agonist GR64349 in isolated guinea pig trachea (pA2 = 8.7). In vivo GR159897 (0.12 mg/kg) inhibits GR64349-induced bronchoconstriction in anesthetized guinea pigs. GR159897 (0.2-50 µg/kg) increases the amount of time spent in the front of the cage during confrontation with a human observer, a marker of anxiolytic-like activity, in marmosets.{60142}
Brand:CaymanSKU:32774 - 1 mgAvailable on backorder
GR159897 is a nonpeptide antagonist of the neurokinin-2 (NK2) receptor.{60141} It binds to NK2 receptors (Ki = 0.32 nM) and is selective for NK2 over NK1 and NK3 receptors in radioligand binding assays (Kis = 5,010 and >1,000 nM, respectively). GR159897 inhibits contractions induced by the NK2 receptor agonist GR64349 in isolated guinea pig trachea (pA2 = 8.7). In vivo GR159897 (0.12 mg/kg) inhibits GR64349-induced bronchoconstriction in anesthetized guinea pigs. GR159897 (0.2-50 µg/kg) increases the amount of time spent in the front of the cage during confrontation with a human observer, a marker of anxiolytic-like activity, in marmosets.{60142}
Brand:CaymanSKU:32774 - 10 mgAvailable on backorder
GR159897 is a nonpeptide antagonist of the neurokinin-2 (NK2) receptor.{60141} It binds to NK2 receptors (Ki = 0.32 nM) and is selective for NK2 over NK1 and NK3 receptors in radioligand binding assays (Kis = 5,010 and >1,000 nM, respectively). GR159897 inhibits contractions induced by the NK2 receptor agonist GR64349 in isolated guinea pig trachea (pA2 = 8.7). In vivo GR159897 (0.12 mg/kg) inhibits GR64349-induced bronchoconstriction in anesthetized guinea pigs. GR159897 (0.2-50 µg/kg) increases the amount of time spent in the front of the cage during confrontation with a human observer, a marker of anxiolytic-like activity, in marmosets.{60142}
Brand:CaymanSKU:32774 - 5 mgAvailable on backorder
GR24 is a synthetic strigalactone and plant growth regulator.{53559,53560} It stimulates the germination of Striga and Orobanche parasitic weed seeds (EC50s = 5-50 nM).{53559} GR24 increases root-hair length and decreases the number of lateral roots in Arabidopsis.{53560}
Brand:CaymanSKU:-GR79236 is a selective agonist of adenosine A1 receptors (Kis = 3.1 and 1,300 nM for adenosine A1 and A2 receptors, respectively, in rat brain).{47666} GR79236 inhibits cAMP accumulation induced by isoprenaline (isoproterenol; Item No. 15592) in DDT1MF-2 hamster smooth muscle cells (IC50 = 2.6 nM) but only decreases contractility in isolated guinea pig atria with an EC50 value of 1,500 nM. It also inhibits lipolysis induced by norepinephrine (Item No. 16673) in rat adipocytes (EC50 = 0.83 nM).{47667} GR79236 decreases locomotor activity and inhibits DMCM-induced seizures in mice (ED50s = 0.13 and 0.3 mg/kg, respectively).{47666} It also decreases mean blood pressure by 74% in anesthetized rats when administered at a dose of 0.1 mg/kg.
Brand:CaymanSKU:28430 - 1 mgAvailable on backorder
GR79236 is a selective agonist of adenosine A1 receptors (Kis = 3.1 and 1,300 nM for adenosine A1 and A2 receptors, respectively, in rat brain).{47666} GR79236 inhibits cAMP accumulation induced by isoprenaline (isoproterenol; Item No. 15592) in DDT1MF-2 hamster smooth muscle cells (IC50 = 2.6 nM) but only decreases contractility in isolated guinea pig atria with an EC50 value of 1,500 nM. It also inhibits lipolysis induced by norepinephrine (Item No. 16673) in rat adipocytes (EC50 = 0.83 nM).{47667} GR79236 decreases locomotor activity and inhibits DMCM-induced seizures in mice (ED50s = 0.13 and 0.3 mg/kg, respectively).{47666} It also decreases mean blood pressure by 74% in anesthetized rats when administered at a dose of 0.1 mg/kg.
Brand:CaymanSKU:28430 - 10 mgAvailable on backorder
GR79236 is a selective agonist of adenosine A1 receptors (Kis = 3.1 and 1,300 nM for adenosine A1 and A2 receptors, respectively, in rat brain).{47666} GR79236 inhibits cAMP accumulation induced by isoprenaline (isoproterenol; Item No. 15592) in DDT1MF-2 hamster smooth muscle cells (IC50 = 2.6 nM) but only decreases contractility in isolated guinea pig atria with an EC50 value of 1,500 nM. It also inhibits lipolysis induced by norepinephrine (Item No. 16673) in rat adipocytes (EC50 = 0.83 nM).{47667} GR79236 decreases locomotor activity and inhibits DMCM-induced seizures in mice (ED50s = 0.13 and 0.3 mg/kg, respectively).{47666} It also decreases mean blood pressure by 74% in anesthetized rats when administered at a dose of 0.1 mg/kg.
Brand:CaymanSKU:28430 - 25 mgAvailable on backorder
GR79236 is a selective agonist of adenosine A1 receptors (Kis = 3.1 and 1,300 nM for adenosine A1 and A2 receptors, respectively, in rat brain).{47666} GR79236 inhibits cAMP accumulation induced by isoprenaline (isoproterenol; Item No. 15592) in DDT1MF-2 hamster smooth muscle cells (IC50 = 2.6 nM) but only decreases contractility in isolated guinea pig atria with an EC50 value of 1,500 nM. It also inhibits lipolysis induced by norepinephrine (Item No. 16673) in rat adipocytes (EC50 = 0.83 nM).{47667} GR79236 decreases locomotor activity and inhibits DMCM-induced seizures in mice (ED50s = 0.13 and 0.3 mg/kg, respectively).{47666} It also decreases mean blood pressure by 74% in anesthetized rats when administered at a dose of 0.1 mg/kg.
Brand:CaymanSKU:28430 - 5 mgAvailable on backorder
GRA Ex-25 is a glucagon receptor (GCGR) antagonist (IC50s = 55 and 56 nM for the human and rat receptors, respectively).{49499} It inhibits adenylate cyclase activity induced by glucagon (Item No. 24204) with a Ki value of 254 nM.{49500} GRA Ex-25 (3 mg/kg, i.v.) reduces glucagon-induced increases in blood glucose levels in rats.{49499}
Brand:CaymanSKU:29727 - 1 mgAvailable on backorder
GRA Ex-25 is a glucagon receptor (GCGR) antagonist (IC50s = 55 and 56 nM for the human and rat receptors, respectively).{49499} It inhibits adenylate cyclase activity induced by glucagon (Item No. 24204) with a Ki value of 254 nM.{49500} GRA Ex-25 (3 mg/kg, i.v.) reduces glucagon-induced increases in blood glucose levels in rats.{49499}
Brand:CaymanSKU:29727 - 10 mgAvailable on backorder
GRA Ex-25 is a glucagon receptor (GCGR) antagonist (IC50s = 55 and 56 nM for the human and rat receptors, respectively).{49499} It inhibits adenylate cyclase activity induced by glucagon (Item No. 24204) with a Ki value of 254 nM.{49500} GRA Ex-25 (3 mg/kg, i.v.) reduces glucagon-induced increases in blood glucose levels in rats.{49499}
Brand:CaymanSKU:29727 - 25 mgAvailable on backorder
GRA Ex-25 is a glucagon receptor (GCGR) antagonist (IC50s = 55 and 56 nM for the human and rat receptors, respectively).{49499} It inhibits adenylate cyclase activity induced by glucagon (Item No. 24204) with a Ki value of 254 nM.{49500} GRA Ex-25 (3 mg/kg, i.v.) reduces glucagon-induced increases in blood glucose levels in rats.{49499}
Brand:CaymanSKU:29727 - 5 mgAvailable on backorder
Gracillin is a steroidal saponin that has been found in C. speciosus and has diverse biological activities.{43305,43306,43307} It reduces cell growth in a panel of 58 leukemia, non-small cell lung, colon, CNS, prostate, melanoma, ovarian, renal, and breast cancer cell lines (GI50s = 0.58-2.44 μM).{43305} Gracillin reduces growth of fish Ich parasite (I. multifiliis) theronts (EC50 = 0.53 mg/L) and induces 100 and 92.5% mortality of I. multifiliis protomonts and encysted tomonts, respectively, when used at a concentration of 0.8 mg/L.{43306} It decreases the number of I. multifiliis-infected goldfish by approximately 75% when used at a concentration of 1 mg/L in tank water. Gracillin (100 mg/kg) reduces ear edema induced by arachidonic acid (Item No. 90010) in mice.{43307}
Brand:CaymanSKU:11848 - 1 mgAvailable on backorder
Gracillin is a steroidal saponin that has been found in C. speciosus and has diverse biological activities.{43305,43306,43307} It reduces cell growth in a panel of 58 leukemia, non-small cell lung, colon, CNS, prostate, melanoma, ovarian, renal, and breast cancer cell lines (GI50s = 0.58-2.44 μM).{43305} Gracillin reduces growth of fish Ich parasite (I. multifiliis) theronts (EC50 = 0.53 mg/L) and induces 100 and 92.5% mortality of I. multifiliis protomonts and encysted tomonts, respectively, when used at a concentration of 0.8 mg/L.{43306} It decreases the number of I. multifiliis-infected goldfish by approximately 75% when used at a concentration of 1 mg/L in tank water. Gracillin (100 mg/kg) reduces ear edema induced by arachidonic acid (Item No. 90010) in mice.{43307}
Brand:CaymanSKU:11848 - 10 mgAvailable on backorder
Gracillin is a steroidal saponin that has been found in C. speciosus and has diverse biological activities.{43305,43306,43307} It reduces cell growth in a panel of 58 leukemia, non-small cell lung, colon, CNS, prostate, melanoma, ovarian, renal, and breast cancer cell lines (GI50s = 0.58-2.44 μM).{43305} Gracillin reduces growth of fish Ich parasite (I. multifiliis) theronts (EC50 = 0.53 mg/L) and induces 100 and 92.5% mortality of I. multifiliis protomonts and encysted tomonts, respectively, when used at a concentration of 0.8 mg/L.{43306} It decreases the number of I. multifiliis-infected goldfish by approximately 75% when used at a concentration of 1 mg/L in tank water. Gracillin (100 mg/kg) reduces ear edema induced by arachidonic acid (Item No. 90010) in mice.{43307}
Brand:CaymanSKU:11848 - 25 mgAvailable on backorder
Gracillin is a steroidal saponin that has been found in C. speciosus and has diverse biological activities.{43305,43306,43307} It reduces cell growth in a panel of 58 leukemia, non-small cell lung, colon, CNS, prostate, melanoma, ovarian, renal, and breast cancer cell lines (GI50s = 0.58-2.44 μM).{43305} Gracillin reduces growth of fish Ich parasite (I. multifiliis) theronts (EC50 = 0.53 mg/L) and induces 100 and 92.5% mortality of I. multifiliis protomonts and encysted tomonts, respectively, when used at a concentration of 0.8 mg/L.{43306} It decreases the number of I. multifiliis-infected goldfish by approximately 75% when used at a concentration of 1 mg/L in tank water. Gracillin (100 mg/kg) reduces ear edema induced by arachidonic acid (Item No. 90010) in mice.{43307}
Brand:CaymanSKU:11848 - 5 mgAvailable on backorder
Gramicidin is a polypeptide antibiotic mixture of gramicidin A (Item No. 26384), gramicidin B, and gramicidin C originally isolated from B. brevis.{47490} It is also a component of the antibiotic tyrothricin (Item No. 22177).{47491} Gramicidin is active against the Gram-positive bacterium S. aureus but not Gram-negative E. coli.{38058} It also protects mice from Pneumococcus infection in vivo when administered at a dose of 0.002 mg/animal. Gramicidin inhibits growth of bacteria by forming pores and channels in the cell wall, which increases its permeability to monovalent cations.{47490} Formulations containing gramicidin have been used as topical agents in the treatment of bacterial skin infections.
Brand:CaymanSKU:28251 - 250 mgAvailable on backorder
Gramicidin A is a peptide component of gramicidin, an antibiotic mixture originally isolated from B. brevis.{47164} Gramicidin A is a highly hydrophobic channel-forming ionophore that forms channels in model membranes that are permeable to monovalent cations. It induces degradation of hypoxia inducible factor 1 α (HIF-1α) in HEK293 cells and reduces growth in a human renal cell carcinoma mouse xenograft model when administered at a dose of 0.22 mg/kg three times per week.{47165} Gramicidin A has commonly been used to study channel structure and function.{47164}
Brand:CaymanSKU:26384 - 1 mgAvailable on backorder
Gramicidin A is a peptide component of gramicidin, an antibiotic mixture originally isolated from B. brevis.{47164} Gramicidin A is a highly hydrophobic channel-forming ionophore that forms channels in model membranes that are permeable to monovalent cations. It induces degradation of hypoxia inducible factor 1 α (HIF-1α) in HEK293 cells and reduces growth in a human renal cell carcinoma mouse xenograft model when administered at a dose of 0.22 mg/kg three times per week.{47165} Gramicidin A has commonly been used to study channel structure and function.{47164}
Brand:CaymanSKU:26384 - 5 mgAvailable on backorder
Gramine (Item No. 23401) is an analytical reference standard that is categorized as an alkaloid.{38364} It is used as an intermediate in the synthesis of tryptophans and tryptamines. This product is intended for research and forensic applications.
Brand:CaymanSKU:23401 - 5 mgAvailable on backorder
Gramine (Item No. 23401) is an analytical reference standard that is categorized as an alkaloid.{38364} It is used as an intermediate in the synthesis of tryptophans and tryptamines. This product is intended for research and forensic applications.
Brand:CaymanSKU:23401 - 50 mgAvailable on backorder
Granisetron is an antagonist of the serotonin (5-HT) receptor subtype 5-HT3 (Ki = 3.9 nM) with antiemetic activity.{23960,47619} It is selective for 5-HT3 over 5-HT4 receptors (Ki = >1,000 nM).{23960} Granisetron (0.3, 1, and 3 mg/kg, p.o.) increases the latency to first vomiting episode and reduces the number of vomiting episodes in a canine model of emesis induced by cisplatin (Item No. 13119).{47619} It also increases the latency to first vomiting episode and reduces the number of vomiting and retching episodes in a ferret model of emesis induced by doxorubicin (Item No. 15007) and cyclophosphamide (Item No. 13849) when administered at doses of 0.1, 0.3, and 1 mg/kg. Formulations containing granisetron have been used in the prevention of nausea and vomiting associated with chemotherapy.
Brand:CaymanSKU:21239 -Out of stock
Granisetron is an antagonist of the serotonin (5-HT) receptor subtype 5-HT3 (Ki = 3.9 nM) with antiemetic activity.{23960,47619} It is selective for 5-HT3 over 5-HT4 receptors (Ki = >1,000 nM).{23960} Granisetron (0.3, 1, and 3 mg/kg, p.o.) increases the latency to first vomiting episode and reduces the number of vomiting episodes in a canine model of emesis induced by cisplatin (Item No. 13119).{47619} It also increases the latency to first vomiting episode and reduces the number of vomiting and retching episodes in a ferret model of emesis induced by doxorubicin (Item No. 15007) and cyclophosphamide (Item No. 13849) when administered at doses of 0.1, 0.3, and 1 mg/kg. Formulations containing granisetron have been used in the prevention of nausea and vomiting associated with chemotherapy.
Brand:CaymanSKU:21239 -Out of stock
Granisetron-d3 is intended for use as an internal standard for the quantification of granisetron (Item No. 21239) by GC- or LC-MS. Granisetron is an antagonist of the serotonin (5-HT) receptor subtype 5-HT3 (Ki = 3.9 nM) with antiemetic activity.{23960,47619} It is selective for 5-HT3 over 5-HT4 receptors (Ki = >1,000 nM).{23960} Granisetron (0.3, 1, and 3 mg/kg, p.o.) increases the latency to a first vomiting episode and reduces the number of vomiting episodes in a canine model of emesis induced by cisplatin (Item No. 13119).{47619} It also increases the latency to a first vomiting episode and reduces the number of vomiting and retching episodes in a ferret model of emesis induced by doxorubicin (Item No. 15007) and cyclophosphamide (Item No. 13849) when administered at doses of 0.1, 0.3, and 1 mg/kg. Formulations containing granisetron have been used in the prevention of nausea and vomiting associated with chemotherapy.
Brand:CaymanSKU:31786 - 1 mgAvailable on backorder
Graphislactone A is an antioxidant produced by Cephalosporium IFB-E001 and M. olivacea.{38444,38445} It exhibits dose-dependent scavenging activity against DPPH radicals and metal ion-dependent hydroxyl radicals in vitro.{38444} Graphislactone A reduces peroxidation of human LDL and slows peroxidation of linoleic acid (Item Nos. 90150 | 21909) by 4.4-fold. It also inhibits acetylcholinesterase (AChE) with an IC50 value of 27 μM.{38445}
Brand:CaymanSKU:23643 - 1 mgAvailable on backorder
Graphislactone A is an antioxidant produced by Cephalosporium IFB-E001 and M. olivacea.{38444,38445} It exhibits dose-dependent scavenging activity against DPPH radicals and metal ion-dependent hydroxyl radicals in vitro.{38444} Graphislactone A reduces peroxidation of human LDL and slows peroxidation of linoleic acid (Item Nos. 90150 | 21909) by 4.4-fold. It also inhibits acetylcholinesterase (AChE) with an IC50 value of 27 μM.{38445}
Brand:CaymanSKU:23643 - 5 mgAvailable on backorder
Grassofermata is an inhibitor of fatty acid transport.{43557} It inhibits C1-BODIPY-C12 uptake in HepG2, Caco-2, C2C12, and INS-1E cells (IC50s = 8.1-10.6 μM).{43557} Grassofermata prevents palmitate-mediated lipid accumulation and cell death in HepG2 cells and primary hepatocytes. In vivo, grassofermata (300 mg/kg) decreases absorption of 13C-oleate in mice.
Brand:CaymanSKU:26202 - 1 mgAvailable on backorder
Grassofermata is an inhibitor of fatty acid transport.{43557} It inhibits C1-BODIPY-C12 uptake in HepG2, Caco-2, C2C12, and INS-1E cells (IC50s = 8.1-10.6 μM).{43557} Grassofermata prevents palmitate-mediated lipid accumulation and cell death in HepG2 cells and primary hepatocytes. In vivo, grassofermata (300 mg/kg) decreases absorption of 13C-oleate in mice.
Brand:CaymanSKU:26202 - 10 mgAvailable on backorder
Grassofermata is an inhibitor of fatty acid transport.{43557} It inhibits C1-BODIPY-C12 uptake in HepG2, Caco-2, C2C12, and INS-1E cells (IC50s = 8.1-10.6 μM).{43557} Grassofermata prevents palmitate-mediated lipid accumulation and cell death in HepG2 cells and primary hepatocytes. In vivo, grassofermata (300 mg/kg) decreases absorption of 13C-oleate in mice.
Brand:CaymanSKU:26202 - 25 mgAvailable on backorder
Grassofermata is an inhibitor of fatty acid transport.{43557} It inhibits C1-BODIPY-C12 uptake in HepG2, Caco-2, C2C12, and INS-1E cells (IC50s = 8.1-10.6 μM).{43557} Grassofermata prevents palmitate-mediated lipid accumulation and cell death in HepG2 cells and primary hepatocytes. In vivo, grassofermata (300 mg/kg) decreases absorption of 13C-oleate in mice.
Brand:CaymanSKU:26202 - 5 mgAvailable on backorder
Grazoprevir is a pan-genotypic protease inhibitor that binds to hepatitis C virus (HCV) non-structural protein 3/4A (NS3/4A), a serine protease essential for viral replication.{36012} Grazoprevir has potent in vitro activity against major HCV genotypes (Kis = 0.1, 0.1, 0.08, 0.15, and 0.9 nM for genotypes 1a, 1b, 2a, 2b, and 3a, respectively) and common resistance genotypes (Kis = 0.07, 0.14, and 0.30 nM for genotypes 1b R155K, D165V, and D168Y, respectively). Grazoprevir inhibits the NS3/4A protease in an in vitro replicon system with EC50 values of 2 and 8 nM for genotypes 1a and 2a, respectively. Formulations containing grazoprevir are used in combination therapies to treat HCV.{36013}
Brand:CaymanSKU:21816 -Out of stock
Grazoprevir is a pan-genotypic protease inhibitor that binds to hepatitis C virus (HCV) non-structural protein 3/4A (NS3/4A), a serine protease essential for viral replication.{36012} Grazoprevir has potent in vitro activity against major HCV genotypes (Kis = 0.1, 0.1, 0.08, 0.15, and 0.9 nM for genotypes 1a, 1b, 2a, 2b, and 3a, respectively) and common resistance genotypes (Kis = 0.07, 0.14, and 0.30 nM for genotypes 1b R155K, D165V, and D168Y, respectively). Grazoprevir inhibits the NS3/4A protease in an in vitro replicon system with EC50 values of 2 and 8 nM for genotypes 1a and 2a, respectively. Formulations containing grazoprevir are used in combination therapies to treat HCV.{36013}
Brand:CaymanSKU:21816 -Out of stock
Grazoprevir is a pan-genotypic protease inhibitor that binds to hepatitis C virus (HCV) non-structural protein 3/4A (NS3/4A), a serine protease essential for viral replication.{36012} Grazoprevir has potent in vitro activity against major HCV genotypes (Kis = 0.1, 0.1, 0.08, 0.15, and 0.9 nM for genotypes 1a, 1b, 2a, 2b, and 3a, respectively) and common resistance genotypes (Kis = 0.07, 0.14, and 0.30 nM for genotypes 1b R155K, D165V, and D168Y, respectively). Grazoprevir inhibits the NS3/4A protease in an in vitro replicon system with EC50 values of 2 and 8 nM for genotypes 1a and 2a, respectively. Formulations containing grazoprevir are used in combination therapies to treat HCV.{36013}
Brand:CaymanSKU:21816 -Out of stock