AMG 837 hemicalcium,1291087-14

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AMG 837 hemicalcium

CAS No. : 1291087-14-3

MCE 国际站：AMG 837 hemicalcium

产品活性：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。

研究领域：GPCR/G Protein

作用靶点：Free Fatty Acid Receptor

In Vitro: 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.

In Vivo: 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 C_max of 1.4 µM.

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