FXR/HSD17B13-modulator-2
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.
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- Formule: C27H24Cl2N2O5S
- Masse moléculaire:559.46
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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 (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.
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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]
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Dosage:5 mg/kg; 10 mg/kg; 20 mg/kg
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Administration:p.o.; daily; 4 weeks (week 8 to week 12, dose adjusted every 5 days based on body weight)
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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.
Chemical Information
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Masse moléculaire 559.46
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Formule C27H24Cl2N2O5S
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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
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
FXR/HSD17B13-modulator-2 Related Classifications
HY-183309 Related Classifications
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