Obeticholic acidCAS号： 459789-99-2分子式： C26H44O4分子量： 420.63描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)参考文献
| 产品描述 | |
| 描述 |
INT-747(Obeticholic acid; 6-ECDCA) is a potent and selective FXR agonist(EC50=99 nM) endowed with anticholestatic activity. |
| 纯度 |
>98%
|
| 储存/保存方法 |
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
|
| 基本信息 | |
| 别名 |
奥贝胆酸; INT-747； 6-ECDCA；6-Ethylchenodeoxycholic acid
|
| 外观 |
white powder
|
| 可溶性/溶解性 |
DMSO：84 mg/mL (199.7 mM)
Ethanol：84 mg/mL warmed (199.7 mM) |
| 生物活性 | |
| 靶点 |
FXR
|
| In vitro(体外研究) |
In HuH7 cells, Obeticholic Acid acts as a potent FXR agonist with EC50 of 85 nM.
|
| In vivo(体内研究) |
In rat cholestasis model, Obeticholic Acid promotes bile flow, and protects hepatocytes against acute necrosis caused by LCA. Obeticholic Acid (p.o.) improves proteinuria, ameliorates renal structural changes, and modulates renal inflammation and oxidative stress in WD-fed DBA mice. In thioacetamide (TAA)-intoxicated and bile-duct-ligated (BDL) rats, Obeticholic Acid (30 mg/kg p.o.) reactivates the FXR downstream signaling pathway and decreases portal pressure by lowering total IHVR without deleterious systemic hypotension.
|
| 参考文献 | |
| 参考文献 |
[1] Pellicciari R, et al. J Med Chem. 2002, 45(17), 3569-3572.
[2] Wang XX, et al. Am J Physiol Renal Physiol. 2009, 297(6), F1587-1596. [3] Verbeke L, et al. Hepatology. 2014, 59(6), 2286-2298. |
分子结构图
