FXR agonist 17
FXR agonist 17 is an orally active, steroidal FXR agonist with EC50 values of 42.2 nM (TR-FRET) and 176.4 nM (luciferase reporter assay), respectively. FXR agonist 17 activates TGR5 (EC50 = 2.6 μM) but does not activate hMRGPRX4. FXR agonist 17 exerts anti-inflammatory, hepatoprotective and antifibrotic effects, improves the non-alcoholic steatohepatitis (NAFLD) activity score and reduces the severity of liver fibrosis. FXR agonist 17 can be used for the research of NAFLD, cholestatic liver disease and liver fibrosis.
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- CAS No.: 3107769-23-0
- Formule: C29H46N2O3S
- Masse moléculaire:502.75
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
Description
In Vitro
FXR agonist 17 (Compound 10) (0.5-100 μM; 25 h) shows no cytotoxicity against RAW264.7 murine macrophages at concentrations ≤ 40 μM, but reduces cell viability at concentrations ≥ 60 μM[1].
FXR agonist 17 (5-20 μM; 25 h) dose-dependently alleviates LPS (HY-D1056)-induced inflammatory responses in RAW264.7 mouse macrophages via FXR activation. Its prominent effects include reducing nitrite, TNF-α and ROS levels, as well as regulating the expression of bile acid metabolism- and inflammation-related genes[1].
FXR agonist 17 (0-500 μM; 25 h) exhibits IC50 values of 62.2 μM, 57 μM, and 46.3 μM in HEK-293, HepG2, and HEK-293 T cells, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RAW264.7 mouse macrophages
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Concentration:0.5, 1, 2, 5, 10, 20, 40, 60, 80, 100 μM
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Incubation Time:1 h pretreatment; 24 h LPS stimulation
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Result:Showed no significant decrease in cell viability at concentrations ≤ 40 μM; showed significant cytotoxicity at 60, 80, and 100 μM.
Parmacokinetics
In Vivo
FXR agonist 17 (Compound 10) (20 mg/kg; p.o.; daily; 28 days) significantly reduces liver fibrosis in CCl4-challenged male C57BL/6 mice, lowering hepatic collagen-positive staining area to 1.48%[1].
FXR agonist 17 (Compound 10) (20 mg/kg; p.o.; daily; 28 days, administered during weeks 8-12 of 12-week induction period) significantly improves hepatic pathology in male C57BL/6 mice, lowering the NAS score to 4.0 and hepatic collagen-positive staining area to 1.75%[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, 6-8 weeks old, SPF-grade, ANIT-induced)[1]
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Dosage:20 mg/kg
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Administration:p.o.; daily; 5 days
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Result:Significantly reduced serum levels of ALP, TBA, and TBIL relative to the ANIT-induced group.
Reduced liver injury as evidenced by decreased cellular necrosis, inflammatory infiltration, and hemorrhage on H&E staining.
Lowered average H&E liver injury score to 4.0, compared to 6.2 in the ANIT-induced group.
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Animal Model:C57BL/6 (male, 6-8 weeks old, SPF-grade, CCl4-induced)[1]
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Dosage:20 mg/kg
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Administration:p.o.; daily; 28 days
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Result:Significantly reduced serum levels of TBA and TBIL relative to the CCl4-induced group.
Reduced hepatic collagen accumulation, with Sirius red-positive staining area decreasing to 1.48% from 1.98% in the CCl4-induced group.
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Animal Model:C57BL/6 (male, 6-8 weeks old, SPF-grade, high-sugar high-fat diet + CCl4-induced)[1]
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Dosage:20 mg/kg
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Administration:p.o.; daily; 28 days (administered during weeks 8-12 of 12-week induction period)
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Result:Significantly reduced serum levels of TC, HDL, and LDL relative to the MASH group.
Reduced hepatic triglyceride and total cholesterol levels relative to the MASH group.
Improved liver histopathology with reduced steatosis, lobular inflammation, and hepatocyte ballooning.
Lowered NAFLD activity score (NAS) to 4.0 from 5.9 in the MASH group.
Reduced hepatic collagen accumulation, with Sirius red-positive staining area decreasing to 1.75% from 2.55% in the MASH group.
Chemical Information
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CAS No. 3107769-23-0
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Masse moléculaire 502.75
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Formule C29H46N2O3S
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SMILES
[H][C@@]12C[C@@H](CC[C@@]1([C@]3(CC[C@@]4([C@H](CC[C@]4([C@@]3([C@@H]([C@@H]2CC)O)[H])[H])[C@@H](CCC5=CC(O)=NC(S)=N5)C)C)[H])C)O
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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 agonist 17 Related Classifications
HY-182026 Related Classifications
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Keywords
- FXR agonist 17
- 3107769-23-0
- FXR agonist17
- FXR agonist-17
- FXR
- G protein-coupled Bile Acid Receptor 1
- TNF Receptor
- Reactive Oxygen Species (ROS)
- C57BL/6 mice
- hMRGPRX4
- cholestatic liver disease
- RAW264.7 mouse macrophages
- liver fibrosis
- metabolic dysfunction-associated steatohepatitis
- CHO-K1 cells
- HEK-293 cells
- NAFLD
- Inhibitor
- inhibitor
- inhibit