2. Metabolic Enzyme/Protease
  3. FXR
  4. 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).

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FXR agonist 13

FXR agonist 13 Chemical Structure

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FXR agonist 13 Related Antibodies

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Description

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)[1].

In Vitro

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.

FXR agonist 13 Related Antibodies
In Vivo

FXR agonist 13 (Compound E2) (3-30 mg/kg, p.o., once daily for 4 weeks) effectively improves hepatic steatosis, inflammation, and fibrosis in obese and MASH mouse models by inhibiting lipid production and inflammatory pathways[1].

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

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].
Dosage: 3 mg/kg, 10 mg/kg, 30 mg/kg
Administration: P.o., once daily for 4 weeks
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.
Molecular Weight

533.90

Formula

C26H20ClF4N3O3
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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References
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FXR agonist 13 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 agonist 13FXR agonist13FXR agonist-13FXRNR1H4MASHScaffold hopping strategyIndazole scaffoldStructure-activity relationshipsInhibitorinhibitorinhibit

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