2. Metabolic Enzyme/Protease PI3K/Akt/mTOR Epigenetics
  3. FXR AMPK
  4. 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.

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FXR antagonist 4

FXR antagonist 4 Chemical Structure

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FXR antagonist 4 Related Antibodies

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Description

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[1].

In Vitro

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.

FXR antagonist 4 Related Antibodies

Real Time qPCR[1]

Cell Line: HepG2 cells
Concentration: 1-10 μM
Incubation Time: 24 h
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.
In Vivo

FXR modulator 1 (compound 4l) (25-100 mg/kg; p.o.; daily; 12 weeks) dose-dependently ameliorates hepatic steatosis, ballooning degeneration, fibrosis, and dyslipidemia in CDA-HFD-induced MASH mice, with the 100 mg/kg dose restoring lipid parameters to near-normal levels and reducing the total NAS score to 2.2[1].

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

Animal Model: C57BL/6 (male, MASH induced by CDA-HFD feeding for 3 weeks prior to treatment)[1]
Dosage: 25 mg/kg; 50 mg/kg; 100 mg/kg
Administration: p.o.; daily; 12 weeks
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.
Molecular Weight

416.42

Formula

C25H20O6
SMILES

COC1=CC=CC(CC2=COC3=C(C2=O)C=CC(OCC4=CC=C(C=C4)C(O)=O)=C3)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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FXR antagonist 4 Related Classifications

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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:

FXR antagonist 4FXR antagonist4FXR antagonist-4FXRAMPKNR1H4AMP-activated protein kinasebile acidSRC1-2 co-activator peptideHEK293T cellsCDA-HFD-induced MASH miceAMPK-ACC signaling pathwayFXR-LBDHepG2 cellsmetabolic dysfunction-associated steatohepatitisInhibitorinhibitorinhibit

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