GPCR19 (GPBA receptors, TGR5, GPBAR1, M-BAR) are G protein-coupled receptors (GPCRs) that are activated by bile acids. They are highly expressed in the gallbladder, ileum, and colon, and are important in the regulation of glucose and lipid metabolism, and energy utilization. Diseases associated with GPBAR1 include Sclerosing Cholangitis and Intrahepatic Cholestasis Of Pregnancy. Among its related pathways are Signaling by GPCR and Peptide ligand-binding receptors. Gene Ontology (GO) annotations related to this gene include G protein-coupled receptor activity and G protein-coupled bile acid receptor activity.
SB756050 is a selective TGR5 agonist currently in phase 1clinical trials for the treatment of type 2 diabetes. Learn More
INT-777 is a potent TGR5 agonist with an EC50 of 0.82 μM. Learn More
dual FXR/TGR5 agonist
INT-767 is a dual farnesoid X receptor (FXR)/TGR5 agonist with mean EC50s of 30 and 630 nM, respectively. Learn More
TGR5 Receptor Agonist is a potent TGR5(GPCR19) agonist, showed improved potency in the U2-OS cell assay (pEC50 = 6.8) and in melanophore cells (pEC50 = 7.5). Learn More
SBI-115 is a TGR5 (GPCR19) antagonist. SBI-115 decreases hepatic cystogenesis with polycystic liver diseases via inhibiting TGR5. Learn More