产品
编 号:F749685
分子式:C29H22Cl2N2O5
分子量:549.4
产品类型
结构图
CAS No: 2181834-03-5
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产品详情
生物活性:
HEC96719 is a selective and orally active tricyclic farnesoid X receptor (FXR) agonist with EC50 values of 1.37 and 1.55 nM by time-resolved fluorescence energy transfer (TR-FRET) and luciferase reporter assays, respectively. HEC96719 significantly improves non-alcoholic steatohepatitis (NASH) and liver fibrosis with favorable tissue distribution in liver and intestine. HEC96719 can be used for the research of non-alcoholic steatohepatitis.
体内研究:
HEC96719 (0.5,1.5 和 5 mg/kg;口服,每天 1 次,共 14 天) 通过测定增加成纤维细胞生长因子 15 (FGF15)的水平证明激活了 FXR.HEC96719 (5 mg/kg;口服,1 次) 增加肝胆盐输出泵 (BSEP) 的水平和回肠中 FGF15 的水平。HEC96719 (0.1, 0.3 和 1 mg/kg;口服,每日 1 次,持续 6 周) 显著改善非酒精性脂肪性肝炎 (NASH) 症状。HEC96719 (0.1,0.3 和 1 mg/kg;口服,每日 1 次,持续 4 周) 对改善肝纤维化有效果,且优于奥贝胆酸 (OCA)。Animal Model:Male ob/ob nonalcoholic steatohepatitis (NASH) mouse models
Dosage:0.1, 0.3 and 1 mg/kg
Administration:Oral administration; 0.1, 0.3 and 1 mg/kg, once daily for 6 weeks
Result:Decreased levels of serum alanine aminotransferase (ALT) and liver triglyceride (TG), dose-dependently increased NASH activity and reduced NASH activity score.
Animal Model:Male C57BL/6 liver fibrosis mouse models
Dosage:0.1, 0.3 and 1 mg/kg
Administration:Oral administration; 0.1, 0.3 and 1 mg/kg, once daily for 4 weeks
Result:Decreased levels of serum ALT and TBIL, and reduced fibrosis area.