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。
| Cas No. | 1415407-60-1 |
| 别名 | (4-环丙基-3,4-二氢-1(2H)-喹喔啉基)[4-(2,5-二甲基苯氧基)-3-吡啶基]甲酮 |
| Canonical SMILES | CC1=CC(OC2=CC=NC=C2C(N3C(C=CC=C4)=C4N(C5CC5)CC3)=O)=C(C)C=C1 |
| 分子式 | C25H25N3O2 |
| 分子量 | 399.48 |
| 溶解度 | Soluble in DMSO |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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 |
