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编 号：F052426
分子式：C21H24O6
分子量：372.41
分子式：C21H24O6
分子量：372.41
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CAS No: 116424-69-2
产品详情
生物活性：
Fargesone A is a potent and selective FXR agonist. Fargesone A shows anti-inflammatory activity.
体内研究：
Fargesone A (3 and 30 mg/kg; i.p.; daily for 7 days) 可显著改善胆管结扎 (BDL) 诱导的慢性肝纤维化小鼠模型。Pharmacokinetics parameters of Fargesone A in micet1/2 (h) Tmax (h) Cmax (ng/mL) AUC0-t (ng/mL*h) AUC0-inf (ng/mL*h) MRT0-inf (h) F (%)
i.v. (5 mpk)0.68±0.1-941±57469±13471±140.43±0.13-
p.o. (10 mpk)0.33±0.040.25±0.00104±16101±32102±320.58±0.0710.8±3.2
Animal Model:C57BL/6 mice, bile duct ligation (BDL)-induced chronic liver fibrosis mouse model
Dosage:3 and 30 mg/kg
Administration:IP, once daily for 7 days
Result:Resulted in a lower level of inflammatory infiltrates and a smaller amount of collagen deposition compared to the vehicle group. Reversed BDL-induced sharp increase in total bilirubin level in the serum. Significantly decreased liver mRNA expression of the inflammatory biomarkers interleukin (IL)-6, IL-1β, inducible nitric oxide synthase (iNOS), and prostaglandin-endoperoxide synthase 2 (COX2).
Animal Model:C57BL6/J mice
Dosage:5 or 10 mg/kg
Administration:IV or PO (Pharmacokinetics Analysis)
Result:Showed acceptable PK profiles in general.
体外研究：
Fargesone A (10 μM; 24 h) 以 FXR 依赖的方式减轻人肝脏 WRL68 细胞的肝细胞紊乱。Fargesone A 的激动作用是通过与 FXR 的直接相互作用实现的。
Fargesone A is a potent and selective FXR agonist. Fargesone A shows anti-inflammatory activity.
体内研究：
Fargesone A (3 and 30 mg/kg; i.p.; daily for 7 days) 可显著改善胆管结扎 (BDL) 诱导的慢性肝纤维化小鼠模型。Pharmacokinetics parameters of Fargesone A in micet1/2 (h) Tmax (h) Cmax (ng/mL) AUC0-t (ng/mL*h) AUC0-inf (ng/mL*h) MRT0-inf (h) F (%)
i.v. (5 mpk)0.68±0.1-941±57469±13471±140.43±0.13-
p.o. (10 mpk)0.33±0.040.25±0.00104±16101±32102±320.58±0.0710.8±3.2
Animal Model:C57BL/6 mice, bile duct ligation (BDL)-induced chronic liver fibrosis mouse model
Dosage:3 and 30 mg/kg
Administration:IP, once daily for 7 days
Result:Resulted in a lower level of inflammatory infiltrates and a smaller amount of collagen deposition compared to the vehicle group. Reversed BDL-induced sharp increase in total bilirubin level in the serum. Significantly decreased liver mRNA expression of the inflammatory biomarkers interleukin (IL)-6, IL-1β, inducible nitric oxide synthase (iNOS), and prostaglandin-endoperoxide synthase 2 (COX2).
Animal Model:C57BL6/J mice
Dosage:5 or 10 mg/kg
Administration:IV or PO (Pharmacokinetics Analysis)
Result:Showed acceptable PK profiles in general.
体外研究：
Fargesone A (10 μM; 24 h) 以 FXR 依赖的方式减轻人肝脏 WRL68 细胞的肝细胞紊乱。Fargesone A 的激动作用是通过与 FXR 的直接相互作用实现的。
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