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Obeticholic acid

CAS No. : 459789-99-2

MCE 站：Obeticholic acid

产品活性：Obeticholic acid (INT-747) 是一种有效的，选择性的和口服活性的 FXR 激动剂，EC₅₀ 为 99 nM，并具有抗胆碱和抗炎作用。Obeticholic acid 还可诱导细胞自噬 (autophagy)。

研究领域：Metabolic Enzyme/Protease  |  Autophagy

作用靶点：FXR  |  Autophagy

In Vitro: Obeticholic acid (INT-747) increases the expression of FXR-regulated genes in rat hepatocytes. Obeticholic acid (INT-747) reduces expression of liver JNK-1 ａnd JNK-2. Obeticholic acid (INT-747) (256 μg/mL) shows complete inhibition of bacterial growth in all strains tested. Intestinal permeability remains unaffected after INT-747-addition to an IFN-γ-exposed intestinal epithelium of Caco-2 cells.

In Vivo: Obeticholic acid (INT-747) (10 mg/kg/day) completely reverted cholestasis induced by E₂17α. Administration of Obeticholic acid (INT-747) partially prevents the impairment in total bile acid output caused by E₂17α by increasing the relative abundance of β-MCA ａnd TCDCA ａnd TDCA. Obeticholic acid (INT-747)7 (10 mg/kg) ａnd HS increases the pulmonary congestion in the animals. INT-747 does not improve renal pathology in the HS-fed animals. Obeticholic acid (INT-747) (5 mg/kg) significantly increases survival in BDL rats. Obeticholic acid (INT-747)-treated BDL rats exhibits a significant selective ileal increase in expression of pore-closing claudin-1. Ileal expression of ZO-1 is significantly up-regulated in INT-747-treated BDL rats.

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