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Obeticholic acid

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    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 (auhagy)。


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更新时间:2026/10/7 8:38:06关注度:2581

关键词标签:INT-747

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Obeticholic acid

CAS No. : 459789-99-2

MCE 国际站: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.

相关产品:Natural Product Like Compound Library | Drug Repurposing Compound Library Plus | FDA-Approved Drug Library Plus | FDA-Approved Drug Library Mini | Bioactive Compound Library Plus | Metabolism/Protease Compound Library | FDA-Approved Drug Library | Autophagy Compound Library | Drug Repurposing Compound Library | Diabetes Related Compound Library | Orally Active Compound Library | FDA Approved & Pharmacopeial Drug Library | Drug-Induced Liver Injury (DILI) Compound Library | Forskolin | GW 4064 | T0901317 | Chenodeoxycholic Acid | Guggulsterone | Fexaramine | Gly-β-MCA | Androsterone | Tauro-β-muricholic acid sodium | Sevelamer hydrochloride | Glyco-Obeticholic acid | Tauro-Obeticholic acid

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