| Hazard Information | Back Directory | [Description]
BMS-986118 is a GPR40 full agonist. GPR40 is a G-protein-coupled receptor expressed primarily in pancreatic islets and intestinal L-cells that has been_x000D_
a target of significant recent therapeutic interest for type II diabetes. Activation of GPR40 by partial agonists elicits insulin secretion only in the presence of elevated blood glucose levels, minimizing the risk of hypoglycemia. | [Uses]
BMS-986118 is a potent, orally active, and selective GPR40 agonist with an EC50 of 0.07 μM. BMS-986118 has dual insulinotropic and GLP-1 secretory effects, resulting in robust plasma glucose lowering effects in acute animal models[1]. | [References]
[1] Shi J, et al. Discovery of Potent and Orally Bioavailable Dihydropyrazole GPR40 Agonists. J Med Chem. 2018;61(3):681-694. DOI:10.1021/acs.jmedchem.7b00982 |
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