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抑制劑描述：

產品名稱：INT-747(Obeticholic acid)

產品別名：6-乙基鵝去氧膽酸

英文別名：INT-747;6-ECDCA

靶點：FXR

CAS：459789-99-2

純度：>98%

外觀：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)

體外研究：

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

體內研究：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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