htgr5

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.

TGR5 agonist 9 is a highly selective, orally active allosteric agonist of TGR5, exhibiting EC₅₀ values of 0.48 μM for hTGR5 and 0.49 μM for mTGR5. It recruits β-arrestin 1 (EC₅₀= 78.8 μM) and β-arrestin 2 (EC₅₀= 12.3 μM), and demonstrates enhanced efficacy in cAMP accumulation (EC₅₀= 0.48 μM). In ICR mouse models, TGR5 agonist 9 shows significant hypoglycemic effects, making it a potential candidate for diabetes research.

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].