FXR antagonist 4
FXR antagonist 4 (Compound 4l) is an orally active, selective FXR antagonist with an IC50 of 0.70 μM. FXR antagonist 4 binds to FXR, differentially regulates bile acid and lipid transporter genes, and exerts no effect on gluconeogenesis-related genes. FXR modulator 1 activates the AMPK signaling pathway to inhibit fatty acid synthesis. FXR modulator 1 alleviates hepatic steatosis, ballooning degeneration and fibrosis, and improves dyslipidemia. FXR modulator 1 can be used for research on metabolic dysfunction-associated steatohepatitis.
For research use only. We do not sell to patients.
- Formula: C25H20O6
- Molecular Weight:416.42
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Biological Activity
FXR modulator 1 potently inhibits CDCA-induced FXR activation in HEK293T cells, with an IC50 of 0.70 μM[1].
FXR modulator 1 (10 μM) potently disrupts the recruitment of CDCA-induced SRC1-2 coactivator peptide to purified FXR-LBD, with an inhibition rate of over 90%[1].
FXR modulator 1 (1-10 μM; 24 h) acts as a selective FXR modulator in HepG2 cells, regulating bile acid and lipid metabolism genes (SHP, BSEP, SREBP-1c, CYP7A1) in a dose-dependent manner, with no effect on gluconeogenic genes (PEPCK, G6Pase)[1].
FXR modulator 1 (2-10 μM) activates the AMPK-ACC pathway in cultured cells in a dose-dependent manner, and increases the phosphorylation levels of AMPK and ACC[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2 cells
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Concentration:1-10 μM
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Incubation Time:24 h
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Result:Downregulated mRNA levels of SHP, BSEP, and SREBP-1c when administered alone or with CDCA, completely reversing CDCA-induced SREBP-1c induction at 10 μM.
Dose-dependently upregulated CYP7A1 mRNA levels compared to vehicle control, both alone and with CDCA.
Showed no significant effects on gluconeogenic genes PEPCK and G6Pase, either alone or in combination with CDCA.
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, MASH induced by CDA-HFD feeding for 3 weeks prior to treatment)[1]
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Dosage:25 mg/kg; 50 mg/kg; 100 mg/kg
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Administration:p.o.; daily; 12 weeks
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Result:Dose-dependently reduced elevated alanine transaminase (ALT), aspartate transaminase (AST), triglycerides (TG), total cholesterol (TC), low-density lipoprotein (LDL-C), and hepatic hydroxyproline (Hyp) levels, while increasing high-density lipoprotein (HDL-C) levels; the 100 mg/kg dose restored lipid parameters to near-normal levels.
Dose-dependently reduced the liver-to-body weight ratio to reverse hepatomegaly.
Dose-dependently reduced hepatic macrovesicular steatosis, hepatocellular ballooning, lipid droplet accumulation, and collagen deposition.
Reduced total NAS scores from 5.4 (model group) to 3.6 (25 mg/kg), 3.1 (50 mg/kg), and 2.2 (100 mg/kg); dose-dependently decreased hepatocellular ballooning and steatosis sub-scores.
Chemical Information
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Molecular Weight 416.42
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Formula C25H20O6
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SMILES
COC1=CC=CC(CC2=COC3=C(C2=O)C=CC(OCC4=CC=C(C=C4)C(O)=O)=C3)=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
FXR antagonist 4 Related Classifications
HY-183279 Related Classifications
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