INT-747(Obeticholic acid)

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抑制剂描述：

产品名称：INT-747(Obeticholic acid)

产品别名：6-乙基鹅去氧胆酸

英文别名：INT-747;6-ECDCA

靶点：FXR

CAS：459789-99-2

纯度：>98%

外观：Powder

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -80℃ for six months.

描述：

INT-747(Obeticholic acid; 6-ECDCA) is a potent and selective FXR agonist(EC50=99 nM) endowed with anticholestatic activity.

溶解性：DMSO：84 mg/mL (199.7 mM)
Ethanol：84 mg/mL warmed (199.7 mM)

体外研究：

In HuH7 cells, Obeticholic Acid acts as a potent FXR agonist with EC50 of 85 nM.

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.

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