LY2922470 是一种有效、选择性的，口服有效的 GPR40 激动剂，作用于 人 GPR40、小鼠 GPR40、大鼠 GPR40 的 EC50 值分别为 7 nM、1 nM、3 nM。LY2922470 可降低血糖水平，同时显著增加胰岛素和 GLP-1，具有治疗 2 型糖尿病 (T2DM) 的潜力。
LY2922470 is a potent, selective and orally available agonist of the G protein-coupled receptor 40 (GPR40), with EC50s of 7 nM, 1 nM and 3 nM for human GPR40, mouse GPR40 and rat GPR40, respectively. LY2922470 reduces glucose levels along with significant increases in insulin and GLP-1, is potential for the treatment of type 2 diabetes mellitus (T2DM)[1]. EC50:7 nM (human GPR40), 1 nM (mouse GPR40), 3 nM (rat GPR40)[1]
[1]. Hamdouchi C, et al. The Discovery, Preclinical, and Early Clinical Development of Potent and Selective GPR40 Agonists for the Treatment of Type 2 Diabetes Mellitus (LY2881835, LY2922083, and LY2922470). J Med Chem. 2016 Dec 22;59(24):10891-10916.
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