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编 号：F111497
分子式：C26H21F3O3.1/2Ca
分子量：457.48
分子式：C26H21F3O3.1/2Ca
分子量：457.48
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CAS No: 1291087-14-3
产品详情
生物活性：
AMG 837 hemicalcium is a potent, orally bioavailable and partial agonist of GPR40/FFA1. AMG 837 hemicalcium inhibits specific [3H]AMG 837 binding at the human FFA1 receptor with a pIC50 of 8.13. AMG 837 hemicalcium could enhance insulin secretion and lower glucose levels in rodents.
体内研究：
AMG 837 (0.03-0.3 mg/kg; a single p.o.) improves glucose tolerance and enhances insulin secretion in Sprague-Dawley rats.AMG 837 (0.03-0.3 mg/kg; p.o. once daily for 21 days) reduces glucose levels and increases insulin levels following glucose challenge in vivo.AMG 837 (0.5 mg/kg; p.o.) displays excellent oral bioavailability (F?=?84%) and a total plasma Cmax of 1.4 μM.Animal Model:8-week old Zucker Fatty Rats
Dosage:0.03, 0.1, 0.3 mg/kg
Administration:Oral gavage once daily for 21 days
Result:Decreased glucose AUC values during the glucose tolerance test (GTT) to 7%, 15%, and 25% at 0.03, 0.1 and 0.3 mg/kg, respectively.Increased insulin levels in the mid- and high-dose groups.Not affected body weights during the 21-day treatment.
Animal Model:8-week old Sprague-Dawley rats
Dosage:0.03, 0.1, 0.3 mg/kg
Administration:A single p.o. administration
Result:Reduced the post-prandial glucose with the half-maximal dose of 0.05 mg/kg.
体外研究：
AMG 837 (1 nM-10 μM) stimulates insulin secretion in a glucose-dependent manner with an EC50 of 142±20 nM on islets isolated from mice.AMG 837 stimulates Ca2+ flux with the EC50s of 13.5, 22.6 and 31.7 nM for human, mouse and rat receptors in CHO cells, respectively.
AMG 837 hemicalcium is a potent, orally bioavailable and partial agonist of GPR40/FFA1. AMG 837 hemicalcium inhibits specific [3H]AMG 837 binding at the human FFA1 receptor with a pIC50 of 8.13. AMG 837 hemicalcium could enhance insulin secretion and lower glucose levels in rodents.
体内研究：
AMG 837 (0.03-0.3 mg/kg; a single p.o.) improves glucose tolerance and enhances insulin secretion in Sprague-Dawley rats.AMG 837 (0.03-0.3 mg/kg; p.o. once daily for 21 days) reduces glucose levels and increases insulin levels following glucose challenge in vivo.AMG 837 (0.5 mg/kg; p.o.) displays excellent oral bioavailability (F?=?84%) and a total plasma Cmax of 1.4 μM.Animal Model:8-week old Zucker Fatty Rats
Dosage:0.03, 0.1, 0.3 mg/kg
Administration:Oral gavage once daily for 21 days
Result:Decreased glucose AUC values during the glucose tolerance test (GTT) to 7%, 15%, and 25% at 0.03, 0.1 and 0.3 mg/kg, respectively.Increased insulin levels in the mid- and high-dose groups.Not affected body weights during the 21-day treatment.
Animal Model:8-week old Sprague-Dawley rats
Dosage:0.03, 0.1, 0.3 mg/kg
Administration:A single p.o. administration
Result:Reduced the post-prandial glucose with the half-maximal dose of 0.05 mg/kg.
体外研究：
AMG 837 (1 nM-10 μM) stimulates insulin secretion in a glucose-dependent manner with an EC50 of 142±20 nM on islets isolated from mice.AMG 837 stimulates Ca2+ flux with the EC50s of 13.5, 22.6 and 31.7 nM for human, mouse and rat receptors in CHO cells, respectively.
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