FXR agonist 13
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).
For research use only. We do not sell to patients.
- Formula: C26H20ClF4N3O3
- Molecular Weight:533.90
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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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Help & FAQs
Biological Activity
FXR agonist 13 (Compound E2) (24 h) exhibits potent FXR agonist activity, with an EC50 value of 0.097 μM and a maximum efficacy (Emax) of 92.4% in HEK293T cells[1].
FXR agonist 13 (20 μM, 24 h) has no significant activating effect on LXRα/β, PPARα/γ/δ, PXR, and TGR5 in HEK293T cells[1].
FXR agonist 13 (0.1 μM, 0-60 min) metabolism is mainly handled by CYP3A4/5 and CYP2C8[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | T1/2 | Tmax | Cmax | AUClast | AUCINF_obs |
|---|---|---|---|---|---|---|---|
| Mice | 10 mg/kg | p.o. | 2.8 h | 0.25 h | 18487 ng/mL | 17921 ng·h/mL | 17950 ng·h/mL |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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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].
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Dosage:3 mg/kg, 10 mg/kg, 30 mg/kg
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Administration:P.o., once daily for 4 weeks
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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.
Chemical Information
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Molecular Weight 533.90
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Formula C26H20ClF4N3O3
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SMILES
O=C(C1=CC=C(C=C1)CN(C(C2=NN(C3=C2C=CC=C3Cl)CCC(F)(F)F)=O)CC4=CC(F)=CC=C4)O
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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 agonist 13 Related Classifications
HY-178959 Related Classifications
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