2. Metabolic Enzyme/Protease GPCR/G Protein Apoptosis Immunology/Inflammation NF-κB
  3. FXR G protein-coupled Bile Acid Receptor 1 TNF Receptor Reactive Oxygen Species (ROS)
  4. 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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FXR agonist 17

FXR agonist 17 Chemical Structure

CAS No. : 3107769-23-0

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FXR agonist 17 Related Antibodies

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Description

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[1].

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.

FXR agonist 17 Related Antibodies

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 T1/2 Tmax Cmax AUC0-24 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.
Molecular Weight

502.75

Formula

C29H46N2O3S
CAS No.
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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Room temperature in continental US; may vary elsewhere.
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Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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FXR agonist 17 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 173107769-23-0FXR agonist17FXR agonist-17FXRG protein-coupled Bile Acid Receptor 1TNF ReceptorReactive Oxygen Species (ROS)NR1H4G-protein coupled receptor 19GPCR19TGR5GPBAR1Tumor Necrosis Factor ReceptorTNFRC57BL/6 micehMRGPRX4cholestatic liver diseaseRAW264.7 mouse macrophagesliver fibrosismetabolic dysfunction-associated steatohepatitisCHO-K1 cellsHEK-293 cellsNAFLDInhibitorinhibitorinhibit

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