Potent and selective GPBA agonist (EC50 = 0.72 nM for hTGR5). Selective for TGR5 over FXR (farnesoid X receptor). Increases plasma GLP-1 levels and reduces blood glucose in mice. Orally available.
Duan et al (2012) Design, synthesis, and antidiabetic activity of 4-phenoxynicotinamide and 4-phenoxypyrimidine-5-carboxamide derivatives as potent and orally efficacious TGR5 agonists. J.Med.Chem. 55 10475 PMID:23148522
















