TGR5 is a G protein-coupled receptor for bile acids that mediates energy balance, inflammation, and digestion. TGR5 Receptor Agonist is a synthetic small molecule activator of this bile acid receptor (pEC50 = 6.8-7.5) that is reported to improve glucagon-like peptide-1 (GLP-1) secretion by increasing intracellular cAMP levels via TGR5. In a canine model, 1 mg/kg of this TGR5 receptor agonist co-administered with glucose has been shown to increase GLP-1 secretion, improving glucose disposal. This compound potently stimulates cAMP formation (EC50 = 2.3 pM) in HEK cells expressing TGR5, and has been used to investigate the signaling, trafficking, and regulation of TGR5 receptors in order to identify potentially useful therapeutics for metabolic disorders.
