2. Metabolic Enzyme/Protease
  3. FXR
  4. Fargesone A

Fargesone A 是一种有效的选择性 FXR 激动剂。Fargesone A 显示抗炎活性。

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Fargesone A Chemical Structure

Fargesone A Chemical Structure

CAS No. : 116424-69-2

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Fargesone A 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Fargesone A is a potent and selective FXR agonist. Fargesone A shows anti-inflammatory activity[1].

IC50 & Target

FXR[1]
体外研究
(In Vitro)

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[1]。
Fargesone A 的激动作用是通过与 FXR 的直接相互作用实现的[1]。

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

Fargesone A 相关抗体:
体内研究
(In Vivo)

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[1]。
Pharmacokinetics parameters of Fargesone A in mice

t1/2 (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±57 469±13 471±14 0.43±0.13 -
p.o. (10 mpk) 0.33±0.04 0.25±0.00 104±16 101±32 102±32 0.58±0.07 10.8±3.2

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

Animal Model: C57BL/6 mice, bile duct ligation (BDL)-induced chronic liver fibrosis mouse model[1]
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[1]
Dosage: 5 or 10 mg/kg
Administration: IV or PO (Pharmacokinetics Analysis)
Result: Showed acceptable PK profiles in general.
分子量

372.41

Formula

C21H24O6
CAS 号
结构分类
初始来源
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

Fargesone A 相关分类

  • 摩尔计算器

  • 稀释计算器

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× = ×
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Fargesone A116424-69-2FXRNR1H4IL-1βiNOSIL-6COX2WRL68Inhibitorinhibitorinhibit

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