FXR/HSD17B13-modulator-2

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FXR/HSD17B13-modulator-2 is a dual FXR activator and HSD17B13 inhibitor with human FXR EC₅₀ of 128 nM, human HSD17B13 IC₅₀ of 0.18 μM, high selectivity over related nuclear receptors and HSD17B isoforms, and oral effectiveness.FXR/HSD17B13-modulator-2 alleviates fatty liver, regulates lipid metabolism, reduces inflammation, and attenuates hepatic fibrosis.FXR/HSD17B13-modulator-2 is the first non-carboxylic acid dual FXR/HSD17B13 modulator.FXR/HSD17B13-modulator-2 can be used for the research of metabolic dysfunction-associated steatohepatitis.

For research use only. We do not sell to patients.

FXR/HSD17B13-modulator-2 Chemical Structure

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Purity & Documentation
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Description

In Vitro

FXR/HSD17B13-modulator-2 (Compound 10) activates FXR in transfected HepG2 cells after 24 h, with an EC₅₀ of 79 nM^[1].
FXR/HSD17B13-modulator-2 exhibits high selectivity for FXR and HSD17B13, with no detectable activity against other HSD17B subtypes or 17 nuclear receptors at a concentration of 10 μM^[1].

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

In Vivo

FXR/HSD17B13-modulator-2 (Compound 10) (5-20 mg/kg; p.o.; daily; 4 weeks) dose-dependently alleviates MASH in a WD + CCl₄-induced mouse model by regulating lipid metabolism, inflammation, and fibrosis^[1].
FXR/HSD17B13-modulator-2 (20 mg/kg; p.o.; daily; 5 consecutive days) preferentially accumulates in the liver (liver-to-plasma ratio 14.2) and activates FXR signaling pathways in the liver and ileum of healthy male C57BL/6 mice following 5 days of 20 mg/kg daily oral dosing^[1].

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

Animal Model:	C57BL/6 (male, 8 weeks old, MASH induced via 12 weeks of high-sugar water + high-fat diet + twice weekly intraperitoneal 0.2% CCl₄ injection)^[1]
Dosage:	5 mg/kg; 10 mg/kg; 20 mg/kg
Administration:	p.o.; daily; 4 weeks (week 8 to week 12, dose adjusted every 5 days based on body weight)
Result:	Dose-dependently reduced NAFLD Activity Score (NAS) and alleviated histopathological MASH features including steatosis, lobular inflammation, and hepatocyte ballooning. Showed efficacy comparable to obeticholic acid at 20 mg/kg when dosed at 20 mg/kg. Dose-dependently reduced hepatic injury markers (ALT, AST, ALP, TBIL, TBA), serum lipid levels, liver lipid levels, liver hydroxyproline, and inflammatory factor levels (IL-6, IL-1β, TNFα). Downregulated pro-fibrotic cytokine TGF-β.

Molecular Weight

559.46

Formula

C₂₇H₂₄Cl₂N₂O₅S

SMILES

ClC1=CC=CC(Cl)=C1C2=NOC(C(C)C)=C2COC3=CC=C(C4=CC=C(C(NS(=O)(C)=O)=O)C=C4)C=C3

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

Handling Instructions (2659 KB)

References

[1]. Xu X, et al. Discovery of the first-in-class highly potent FXR/HSD17B13 dual modulator for the treatment of metabolic dysfunction-associated steatohepatitis. Bioorg Chem. 2026;176:109843.