4-IsoxazolecarboxaMide, 3-(2-chlorophenyl)-N-(4-chlorophenyl)-N,5-diMethyl-

TGR5 receptor agonist is an agonist of the bile acid G protein-coupled receptor TGR5 (EC₅₀s = 31.6-158.5 nM in cell-based assays). It stimulates cAMP formation in HEK293 cells expressing TGR5 (EC₅₀ = 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 (IC₅₀s = 316.2 and 1,259 nM, respectively).