TGR5 Receptor Agonist

Description: TGR5 Receptor Agonist is a novel, potent and synthetic small molecule agonist of TGR5(G-protein coupled receptor19, GPCR19) agonist, it showed improved potency in the U2-OS cell assay with pEC50 of 6.8 and in melanophore cells with pEC50 of 7.5. TGR5 Receptor Agonist is 3-aryl-4-isoxazolecarboxamide analog identified from a high-throughput screening campaign as novel, potent small molecule agonists of the human TGR5 G-protein coupled receptor is described. TGR5 Receptor Agonist demonstrated improved GLP-1 secretion in vivo via an intracolonic dose coadministered with glucose challenge in a canine model. G-protein coupled receptor is potentially useful therapeutics for metabolic disorders such as type II diabetes and its associated complications.

References: J Med Chem. 2009 Dec 24; 52(24):7962-5