F44-S101
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. F44-S101 decreases total cholesterol, triglyceride and low-density lipoprotein cholesterol levels. F44-S101 can be used in studies related to hyperlipidemia.
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- No. CAS: 3124701-00-1
- Fòrmula: C27H25ClN2O6S2
- Peso molecular:573.08
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
F44-S101 (10-100 mg/kg; intragastric; 4 weeks) dose-dependently reduces serum TC, hepatic TC, serum LDL-C, inguinal adipose mass, and serum ceramide levels in HFD-induced hyperlipidemic male C57BL/6 mice, with the 100 mg/kg dose decreasing serum TC by 25.6% and hepatic TC by 17.3%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (male, 8 weeks old; Triton WR-1339-induced acute hyperlipidemia)[1]
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Dosage:10 mg/kg; 30 mg/kg; 100 mg/kg
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Administration:intragastric
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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.
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Animal Model:C57BL/6 (male, adult; high-fat diet-induced hyperlipidemia)[1]
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Dosage:10 mg/kg; 30 mg/kg; 100 mg/kg
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Administration:intragastric; 4 weeks
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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.
Chemical Information
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No. CAS 3124701-00-1
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Peso molecular 573.08
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Fòrmula C27H25ClN2O6S2
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SMILES
CCN(S(=O)(C1=CC2=C(SC(C(O)=O)=C2)C=C1)=O)C3=CC=C(C=C3CN(C(C4CC4)=O)CC5=CC=CO5)Cl
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
F44-S101 Related Classifications
HY-181876 Related Classifications
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