1. Discovery of a novel potent GPR40 full agonist.
- Author
-
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, and Player, Mark R.
- Subjects
- *
G protein coupled receptors , *DRUG development , *DRUG efficacy , *INSULIN , *GLUCOSE - Abstract
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. [ABSTRACT FROM AUTHOR]
- Published
- 2018
- Full Text
- View/download PDF