amg-837

AMG 837 是一种新型高效的 GPR40 FFA1激动剂，可增强啮齿动物的胰岛素分泌并降低血糖水平。

(Rac)-AMG8379 ((Rac)-AMG8380) 是 AMG8379 的外消旋体，是一种具有口服活性和选择性的磺胺 NaV1.7 拮抗剂。

AMG 837 sodium salt is a potent GPR40 agonist(EC50=13 nM) with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents. IC50 value: 13 nM (EC50) [1] Target: GPR40 agonist AMG 837 displayed the expected t

AMG 837 hemicalcium 是一种有效的、口服具有活力的 GPR40 FFA1部分激动剂。AMG 837 hemicalcium 能够抑制 [3H]AMG 837 与人类 FFA1受体的特异性结合 (pIC50: 8.13)。AMG 837 hemicalcium 能够提高啮齿动物的胰岛素分泌，减少葡萄糖水平。

AMG 837 calcium hydrate 是口服有效的 GPR40 FFA1部分激动剂，抑制 [3H]AMG 837 与人类 FFA1受体的特异性结合，pIC50为 8.13。AMG 837 calcium hydrate 可增强啮齿动物的胰岛素分泌并降低葡萄糖水平。

AM-3189 is a potent and selective GPR40 Agonist with minimal CNS penetration, superior pharmacokinetic properties and in vivo efficacy comparable to AMG 837. AM-3189 maintains the in vivo efficacy of AMG 837 while displaying a superior pharmacokinetic profile and minimal CNS exposure. Similar to AMG 837, while highly potent on GPR40, AM-3189 was highly selective over the closely related GPCRs, GPR41 and GPR43. 13kdemonstrated low clearance, moderate volume of distribution, and good oral bioavailability. AM-3189 does not penetrate the rat CNS as indicated by a rat brain to plasma ratio of 0.04 at 3 h after an oral dose of 5 mg kg.