2. Metabolic Enzyme/Protease
  3. FXR
  4. FXR agonist 13

FXR agonist 13 是一种选择性强、口服有效的高效 FXR 激动剂 (EC50 = 0.097 μM)，且具有良好的肝微粒体代谢稳定性。FXR agonist 13 与 FXR-LBD 直接结合后表现出中等亲和力 (KD = 14.74 μM)。FXR agonist 13 对相关核受体，包括 LXRα/β、PPARα/γ/δ、PXR 和 TGR5，均表现出良好的选择性。FXR agonist 13 可用于代谢相关性脂肪性肝炎 (MASH) 的研究。

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FXR agonist 13

FXR agonist 13 Chemical Structure

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FXR agonist 13 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FXR agonist 13 is a selective, orally active, potent FXR agonist (EC50 = 0.097 μM) and has favorable hepatic microsomal metabolic stability. FXR agonist 13 exhibits moderate affinity for FXR-LBD upon direct binding (KD = 14.74 μM). FXR agonist 13 displays good selectivity against related nuclear receptors, including LXRα/β, PPARα/γ/δ, PXR, and TGR5. FXR agonist 13 can be used for the study of metabolic-associated steatohepatitis (MASH)[1].

体外研究
(In Vitro)

FXR agonist 13 (Compound E2) (24 小时) 表现出强效的 FXR 激动剂活性，在 HEK293T 细胞中 EC50 值为 0.097 μM，最大效力 (Emax) 为 92.4 %[1]。
FXR agonist 13 (20 μM，24 小时) 对 HEK293T 细胞中的 LXRα/β、PPARα/γ/δ、PXR 和 TGR5 没有显著的激活作用[1]。
FXR agonist 13 (0.1 μM，0-60 分钟) 的代谢主要由 CYP3A4/5 和 CYP2C8 负责[1]。

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

FXR agonist 13 相关抗体:
体内研究
(In Vivo)

FXR agonist 13 (Compound E2) (3-30 mg/kg，口服，每日一次，持续 4 周) 通过抑制脂质生成和炎症通路，有效改善肥胖和 MASH 小鼠模型的肝脂肪变性、炎症和纤维化[1]。

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

Animal Model: Obesity and MASH models were induced in male C57BL/6J mice (6 weeks old, initial weight 18-22 g) by feeding them a high-fat diet (HFD, 60% of calories from fat) for 12 weeks[1].
Dosage: 3 mg/kg, 10 mg/kg, 30 mg/kg
Administration: P.o., once daily for 4 weeks
Result: No significant improvement in body weight, but a significant decrease in liver weight ratio, indicating a reduction in liver lesions.
Improved liver appearance; H&E staining showed reduced steatosis and hepatocellular damage.
Significantly reduced serum ALT and AST levels(10 mg/kg).
Reduced serum total cholesterol (TC) levels, but had little effect on high-density lipoprotein (HDL).
Significantly reduced hepatic triglyceride (TG) and total cholesterol (TC) levels.
Significantly reduced HYP content, downregulated lipogenesis-related genes (SREBP-1c and ACC-1), but did not affect FGF15 expression.
分子量

533.90

Formula

C26H20ClF4N3O3
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 13 相关分类

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  • 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:

FXR agonist 13FXR agonist13FXR agonist-13FXRNR1H4MASHScaffold hopping strategyIndazole scaffoldStructure-activity relationshipsInhibitorinhibitorinhibit

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