2. Metabolic Enzyme/Protease
  3. FXR
  4. FXR agonist 15

FXR agonist 15 是一种选择性、强效且有口服活性的法尼酯 X 受体 (FXR) 激动剂，其 EC50 值为 0.76 μM。FXR agonist 15 对其他核受体，包括 LXRα/β、PXR、PPARα/β/γ 和 THR-β 无明显激活作用，其 EC50 均大于 10 μM。FXR agonist 15 可减轻脂肪变性、小叶炎症、肝细胞气球样变和肝纤维化。FXR agonist 15 可用于非酒精性脂肪性肝炎 (NASH) 的研究。

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FXR agonist 15

FXR agonist 15 Chemical Structure

CAS No. : 2991276-14-1

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FXR agonist 15 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

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生物活性

FXR agonist 15 is a selective, potent and orally active farnesoid X receptor (FXR) agonist with EC50 of 0.76 μM. FXR agonist 15 exhibits no obvious activation on other nuclear receptors including LXRα/β, PXR, PPARα/β/γ, THR-β, with EC50 values all >10 μM. FXR agonist 15 can alleviate steatosis, lobular inflammation, hepatocyte ballooning and liver fibrosis. FXR agonist 15 can be used for the research of nonalcoholic steatohepatitis (NASH)[1].

体内研究
(In Vivo)

FXR agonist 15 (Compound 19) (20 mg/kg, 灌胃，每天一次，持续 4 周) 可缓解西方饮食和 CCl4 (HY-Y0298) 诱导的 NASH，减少肝脏脂肪变性、炎症和纤维化[1]
FXR agonist 15 (500 mg/kg，口服，每天一次，持续 10 天) 在 ICR 小鼠中无小鼠死亡及异常行为，血清肝肾功能指标 (AST、ALT、ALP、肌酐、尿素)、血脂指标 (TG、TC) 无显著异常，主要脏器无急性毒性损伤，安全性良好[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: WD + CCl4-induced mice NASH models (C57BL/6, 8 weeks)[1]
Dosage: 20 mg/kg 
Administration: Orally gavage, per day for 4 weeks
Result: Reduced hepatic lipid droplets, NAFLD activity score (NAS), and levels of triacylglycerol (TG) and total cholesterol (TC).
Decreased fibrotic markers (α-SMA, hydroxyproline) and activated the FXR pathway.
Upregulated SHP, BSEP, and OSTβ, while downregulated CYP7A1.
分子量

526.40

Formula

C24H22Cl2FNO5S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

FXR agonist 15 相关分类

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Keywords:

FXR agonist 152991276-14-1FXR agonist15FXR agonist-15FXRNR1H4SARNASHFibrosischolesterolSHPBSEPOSTβInhibitorinhibitorinhibit

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