TGR5, also known as GPBAR1, is a G protein-coupled receptor (GPCR) belonging to the bile acid receptor subclass. It is a plasma membrane-bound transmembrane protein and is primarily expressed in spleen and placenta. TGR5 is activated by the endogenous bile acids cholic acid , lithocholic acid , taurolithocholic acid , deoxycholic acid (Item Nos. 20756 | 18231), and chenodeoxycholic acid , among others. Activation of TGR5 by the synthetic agonist INT-777 decreases plasma triglyceride levels and urinary levels of albumin, thiobarbituric acid reactive substances (TBARS), and hydrogen peroxide, as well as prevents diabetic nephropathy, in a db/db mouse model of diabetes. Activation of TGR5 by INT-777 also prevents hepatic steatosis and increases in fat, liver, and brown adipose tissue mass in a mouse model of diet-induced obesity. Transgenic overexpression of TGR5 increases glucose tolerance, as well as plasma levels of insulin and glucagon-like peptide 1 (GLP-1), during an oral glucose tolerance test in mice fed a high-fat diet. Increased expression of TGR5 has been found in tissue samples from patients with intestinal-type adenocarcinoma or intestinal metaplasia, but not healthy mucosa. TGR5 protein levels are also increased in patient-derived Barrett''s esophagous and esophageal adenocarcinoma tissues. Cayman''s TGR5 (C-Term) Polyclonal Antibody can be used for Western blot and immunohistochemistry (IHC) applications. The antibody recognizes the C-terminal region of TGR5 from human samples.
