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Art. -Nr.: HY-182026

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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. Nr.: 3107769-23-0
Formel: C₂₉H₄₆N₂O₃S
Molecular Weight:502.75

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

FXR agonist 17 Chemical Structure

CAS. Nr.: 3107769-23-0

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle TNF Receptor Isoform-spezifische Produkte anzeigen :

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.

Cell Viability Assay^[1]

Cell Line:

RAW264.7 mouse macrophages
Concentration:

0.5, 1, 2, 5, 10, 20, 40, 60, 80, 100 μM
Incubation Time:

1 h pretreatment; 24 h LPS stimulation
Result:

Showed no significant decrease in cell viability at concentrations ≤ 40 μM; showed significant cytotoxicity at 60, 80, and 100 μM.

Parmacokinetics

Species	Dose	Route	Bioavailability	T_1/2	T_max	C_max	AUC_0-24	CL
Rat^[1]	2 mg/kg	i.v.	/	1.27 h	0.0333 h	8210 ng/mL	2540 ng·h/mL	824 mL/h/kg
Rat^[1]	10 mg/kg	p.o.	18.5 %	1.66 h	1.67 h	636 ng/mL	2340 ng·h/mL	3970 mL/h/kg

In Vivo

FXR agonist 17 (Compound 10) (20 mg/kg; p.o.; daily; 5 days) significantly reduces cholestatic liver injury in ANIT-challenged male C57BL/6 mice, lowering the average H&E liver injury score to 4.0^[1].
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.

Animal Model:

C57BL/6 (male, 6-8 weeks old, SPF-grade, ANIT-induced)^[1]
Dosage:

20 mg/kg
Administration:

p.o.; daily; 5 days
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.

Animal Model:

C57BL/6 (male, 6-8 weeks old, SPF-grade, CCl₄-induced)^[1]
Dosage:

20 mg/kg
Administration:

p.o.; daily; 28 days
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.

Animal Model:

C57BL/6 (male, 6-8 weeks old, SPF-grade, high-sugar high-fat diet + CCl₄-induced)^[1]
Dosage:

20 mg/kg
Administration:

p.o.; daily; 28 days (administered during weeks 8-12 of 12-week induction period)
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

CAS. Nr. 3107769-23-0
Molecular Weight 502.75
Formel C₂₉H₄₆N₂O₃S
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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Zheng X, et al. Discovery of a pyrimidine-based steroidal FXR agonist for the treatment of metabolic dysfunction-associated steatotic liver disease. Bioorg Chem. Published online March 4, 2026. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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Biologische Aktivität
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- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
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FXR agonist 17

Alle TNF Receptor Isoform-spezifische Produkte anzeigen