AMG 837 hemicalcium 是GPR40/FFA1的有效的、具有口服活性的部分激动剂，抑制 [3H]AMG 837 与人类FFA1受体的特异性结合，pIC50值为 8.13。AMG 837 hemicalcium 可增强啮齿动物的胰岛素分泌并降低葡萄糖水平。

AMG 837 hemicalcium is a potent, orally bioavailable and partial agonist of GPR40/FFA1. AMG 837 hemicalcium inhibits specific [ 3 H]AMG 837 binding at the human FFA1 receptor with a pIC 50 of 8.13. AMG 837 hemicalcium could enhance insulin secretion and lower glucose levels in rodents [1] [2] [3].

AMG 837 (1 nM-10 μM) stimulates insulin secretion in a glucose-dependent manner with an EC 50 of 142±20 nM on islets isolated from mice [1]. AMG 837 stimulates Ca 2+ flux with the EC 50 s of 13.5, 22.6 and 31.7 nM for human, mouse and rat receptors in CHO cells, respectively [1].

AMG 837 (0.03-0.3 mg/kg; a single p.o.) improves glucose tolerance and enhances insulin secretion in Sprague-Dawley rats [1]. 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 [1]. AMG 837 (0.5 mg/kg; p.o.) displays excellent oral bioavailability (F = 84%) and a total plasma C max of 1.4 μM [1]. Animal Model: 8-week old Sprague-Dawley rats [1] 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. Animal Model: 8-week old Zucker Fatty Rats [1] 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.

1291087-14-3

C52H40CaF6O6

914.954

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years