TC-G 1005 是一种强效、选择性和口服活性的 BA 受体 Takeda G 蛋白偶联受体 5 (TGR5) 激动剂，对 hTGR5 和 mTGR5 的 EC50 分别为 0.72 和 6.2 nM。
货号:ajcx26936
CAS:1415407-60-1
分子式:C25H25N3O2
分子量：399.48
溶解度:Soluble in DMSO
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Potent and selective GPBA agonist (EC50 = 0.72 nM for hTGR5). Selective for TGR5 over FXR (farnesoid X receptor). Increases plasma GLP-1 levels and reduces blood glucose in mice. Orally available.

Duan et al (2012) Design, synthesis, and antidiabetic activity of 4-phenoxynicotinamide and 4-phenoxypyrimidine-5-carboxamide derivatives as potent and orally efficacious TGR5 agonists. J.Med.Chem. 55 10475 PMID:23148522