tgr5 receptor agonist

TGR5 is a potent TGR5(GPCR19) agonist.

TGR5 Receptor Agonist 3 is a G protein-coupled bile acid receptor 1 (GPBAR1, TGR5) agonist soft drug compound that decreases gallbladder filling, exhibits good gallbladder safety, and is able to act on hTGR5 (EC50: 16.4 nM) and mTGR5 (EC50: 209 nM).

TGR5 Receptor Agonist 4, a selective agonist for the Bile Acid Receptor (TGR5), exhibits potent activity with an EC50 of 2 nM for human TGR5 (hTGR5) and 3 nM for mouse TGR5 (mTGR5). It is notably involved in mediating hypoglycemic and weight loss effects [1].

INT-767 is a potent farnesoid X receptor (FXR)/TGR5 dual agonist that prevents NASH and promotes visceral adipose brown lipogenesis and mitochondrial function for the study of non-alcoholic steatohepatitis.

Deoxycholic acid (DCA) is a natural product and a TGR5 receptor agonist with cell permeability and oral activity. As a metabolite of intestinal flora, this compound is widely used in research on bile acid signal transduction, glucose and lipid metabolism, and anti-inflammatory mechanisms, and has shown therapeutic potential in diabetes and liver disease models.

TGR5 agonist 7 (Compound 22-Na) is an intestine-restricted, orally active agonist of the G protein-coupled bile acid receptor TGR5 (GPBAR1 or GPR131) with an EC50 of less than 1 μM. In mouse models, it demonstrates blood glucose-lowering effects, making it useful for diabetes research.

GPBAR-A is a synthetic small-molecule agonist of GPBAR1, also known as TGR5, that activates this G protein–coupled bile acid receptor involved in energy homeostasis, glucose metabolism, and immune regulation, GPBAR-A is extensively studied for its therapeutic potential in metabolic disorders such as type 2 diabetes, obesity, and inflammation-related diseases.

TGR5 agonist 4 (compound 19), a cholic acid derivative, selectively activates the TGR5 receptor with an EC50 of 4 μM [1].

TC-G 1005 is a potent and selective GPBA agonist (EC50 :0.72 nM; hTGR5). Selective for TGR5 over FXR (farnesoid X receptor). Increases plasma GLP-1 levels and reduces blood glucose in mice. Orally available.