human gpr40

LY2922470 reduces glucose levels along with significant enhancements in insulin and GLP-1, which is the potential for the treatment of type 2 diabetes mellitus (T2DM). LY2922470 is an effective, selective, and orally available agonist of the G protein-cou

AM-4668, a GPR40 (FFA1) agonist with oral availability, was optimized to reduce central nervous system (CNS) permeability, with a mouse brain/plasma ratio of only 0.02, and significantly reduced blood glucose levels in human GPR40 knock-in mice.

GPR40 agonist 1 is an effective new GPR40 agonist (EC50s: 17 nM and 2 nM for rGPR40 and hGPR40).

K-757 is a GPR40 agonist with an EC50 value of 2.1 ± 0.2 nM for human GPR40. In preclinical species, K-757 has a half-life ranging from 1 to 11 hours. It can stimulate the secretion of GLP-1 and shows potential applications in weight loss studies.

AMG 837 hemicalcium is a potent, orally active GPR40/FFA1 partial agonist that inhibits the specific binding of [3H]AMG 837 to the human FFA1 receptor (pIC50: 8.13). It promotes insulin secretion and reduces glucose levels in rodents.

TP-051 is a potent and selective FFAR1 agonist exhibiting a Ki of 16 nM for human FFAR1, with demonstrated ability to enhance insulin secretion in rat insulinoma cells. TP-051 is widely used as a chemical probe for studying free-fatty-acid receptor-mediated pathways in type 2 diabetes and metabolic research.

TUG-770 is a GPR40/FFA1 agonist with potential anti-inflammatory activity.TUG-770 can be used to study type 2 diabetes, dementia, and Alzheimer's disease.