Description
TGR5 receptor agonist is an agonist of the bile acid G protein-coupled receptor TGR5 (EC
50s = 31.6-158.5 nM in cell-based assays). It stimulates cAMP formation in HEK293 cells expressing TGR5 (EC
50 = 2.3 pM). TGR5 receptor agonist (1 mg/kg) increases glucagon-like peptide 1 (GLP-1) secretion and decreases glucose levels in the hepatic portal vein in dogs when administered in combination with glucose. It also inhibits the cytochrome P450 (CYP) isozymes CYP2C19 and CYP3A4 (IC
50s = 316.2 and 1,259 nM, respectively).