2. Metabolic Enzyme/Protease
  3. FXR
  4. F44-S101

F44-S101 是一种口服有效、强效且选择性的肠道限制性 FXR 拮抗剂，IC50 为 0.48 μM，具有降血脂活性。F44-S101 可选择性拮抗肠道 FXR，反馈激活肝脏 FXR，促进胆固醇代谢并减少脂质蓄积。\nF44-S101 可降低总胆固醇、甘油三酯和低密度脂蛋白胆固醇水平。F44-S101 可用于高脂血症的相关研究。

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F44-S101

F44-S101 Chemical Structure

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Customer Review

F44-S101 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

F44-S101 is an orally active, potent, and selective gut-restricted FXR antagonist with an IC50 of 0.48 μM and lipid-lowering activity. F44-S101 selectively antagonizes intestinal FXR, feedback-activates hepatic FXR, promotes cholesterol metabolism and reduces lipid accumulation.\nF44-S101 decreases total cholesterol, triglyceride and low-density lipoprotein cholesterol levels. F44-S101 can be used in studies related to hyperlipidemia[1].

体外研究
(In Vitro)

F44-S101 是一种强效且具有选择性的肠道限制性 FXR 拮抗剂，其 IC50 值为 0.48 μM[1]。

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

F44-S101 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 Tmax Cmax AUC0-t Vss CL F
Rat[1] 1 mg/kg i.v. 1.60 h 0.08 h 119.24 ng/mL 47.77 ng·h/mL 24.04 L/kg 20.09 L/h/kg /
Rat[1] 10 mg/kg p.o. 2.05 h 0.33 h 160.25 ng/mL 119.50 ng·h/mL / / 25.02 %
体内研究
(In Vivo)

F44-S101 (10-100 mg/kg；灌胃) 可剂量依赖性降低 Triton 诱导的高脂血症雄性 C57BL/6 小鼠的血清 TC、TG 和 LDL-C 水平，并逆转肝酶升高；其中 100 mg/kg 剂量可使血清 TC 降低 18.9%、TG 降低 32.2%[1]。
F44-S101 (10-100 mg/kg；灌胃；4 周) 可呈剂量依赖性降低高脂饮食 (HFD) 诱导的高脂血症雄性 C57BL/6 小鼠的血清 TC、肝脏 TC、血清 LDL-C、腹股沟脂肪量及血清神经酰胺水平；其中 100 mg/kg 剂量可使血清 TC 降低 25.6%，肝脏 TC 降低 17.3%[1]。

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

Animal Model: C57BL/6 (male, 8 weeks old; Triton WR-1339-induced acute hyperlipidemia)[1]
Dosage: 10 mg/kg; 30 mg/kg; 100 mg/kg
Administration: intragastric
Result: Significantly decreased serum total cholesterol (TC) by 18.9% and serum triglycerides (TG) by 32.2% at 100 mg/kg compared to vehicle controls.
Significantly reduced serum low-density lipoprotein cholesterol (LDL-C) levels by over 38% across all dose groups compared to vehicle controls.
Reversed Triton-induced elevations in plasma alanine transaminase (ALT) and aspartate transaminase (AST) levels.
Animal Model: C57BL/6 (male, adult; high-fat diet-induced hyperlipidemia)[1]
Dosage: 10 mg/kg; 30 mg/kg; 100 mg/kg
Administration: intragastric; 4 weeks
Result: Significantly reduced serum TC by 25.6% and hepatic TC by 17.3% at 100 mg/kg compared to vehicle controls.
Significantly reduced plasma LDL-C concentrations by 30.8% at 100 mg/kg compared to vehicle controls, with LDL-C levels approaching control group levels.
Dose-dependently reduced inguinal adipose tissue mass and the ratio of inguinal adipose tissue to body weight; showed a significant reduction in inguinal fat weight at 100 mg/kg compared to vehicle controls.
Significantly reduced serum ceramide levels in a dose-dependent manner compared to vehicle controls.
Had no significant effect on ALT, AST, brown adipose tissue weight, or epididymal fat weight.
分子量

573.08

Formula

C27H25ClN2O6S2
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

F44-S101 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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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:

F44-S101FXRNR1H4male C57BL/6 miceFarnesoid X receptorTriton-induced hyperlipidemic micelipid accumulationlipid metabolic disordersHFD-induced hyperlipidemic micehyperlipidemiaintestinal FXRhepatic FXRcholesterol metabolismInhibitorinhibitorinhibit

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目录号：
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