新型强效GPR40完全激动剂的发现
Discovery of a novel potent GPR40 full agonist.
作者信息
Meegalla Sanath K, Huang Hui, Martin Tonya, Xu June, Zhao Shuyuan, Liu Jianying, Hall Meghan, Gunnet Joe, Wang Yuanping, Rady Brian, Silva Jose, Otieno Monicah, Arnoult Eric, Paul Lee S, Pocai Alessandro, Player Mark R
机构信息
CVM Discovery, Janssen Research & Developmen, LLC, Welsh and McKean Roads, Spring House, PA 19477-0776, USA.
PDS-TPL-TOX, Janssen Research & Development, LLC, Welsh and McKean Roads, Spring House, PA 19477-0776, USA.
出版信息
Bioorg Med Chem Lett. 2018 Feb 15;28(4):720-726. doi: 10.1016/j.bmcl.2018.01.013. Epub 2018 Jan 12.
Compound 12 is a GPR40 agonist that realizes the full magnitude of efficacy possible via GPR40 receptor agonism. In vitro and in vivo studies demonstrated superior glucose lowering by 12 compared to fasiglifam (TAK-875), in a glucose dependent manner. The enhanced efficacy observed with the full agonist 12 was associated with both direct and indirect stimulation of insulin secretion.
化合物12是一种GPR40激动剂，可通过GPR40受体激动作用实现最大程度的疗效。体外和体内研究表明，与法格列净（TAK-875）相比，化合物12能以葡萄糖依赖性方式更有效地降低血糖。全激动剂化合物12所观察到的增强疗效与胰岛素分泌的直接和间接刺激均相关。
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