S217879
S217879 is an orally active and selective NRF2 activator. S217879 activates the NRF2 pathway by specifically disrupting the KEAP1 (Kd: 4.15 nM)-NRF2 interaction, and upregulates the antioxidant response. S217879 also ameliorates steatohepatitis and reduces the degree of liver fibrosis. S217879 can be used in the research of metabolic dysfunction-associated steatotic liver disease and nonalcoholic steatohepatitis.
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- CAS No.: 2700303-28-0
- Formule: C30H32N4O7S
- Masse moléculaire:592.66
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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
Activité biologique
S217879 (0.1-10000 nM) potently induces nuclear translocation of NRF2 in U2OS KEAP1-NRF2 cells, with an EC50 of 23 nM[1].
S217879 (0.1-10000 nM) potently activates ARE-regulated transcription in HepG2 ARE-BLA cells, with an EC50 of 18 nM[1].
S217879 (1 μM; overnight pre-incubation) significantly reduces H2O2-induced ROS production in HepG2 cells[1].
S217879 (0.1-1000 nM; 6 h) potently upregulates the expression of the Nqo1 gene in primary human peripheral blood mononuclear cells (PBMCs), with an EC50 of 16 nM[1].
S217879 (30-1000 nM; 4 h) significantly inhibits LPS (HY-D1056)-induced secretion of IL-1β and MCP-1 in primary human PBMCs, with an IC50 of < 30 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PBMCs treated LPS (HY-D1056)
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Concentration:30,100, 300, 1000 nM
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Incubation Time:4 h pre-incubation
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Result:Significantly inhibited LPS-induced IL-1β and MCP-1 secretion, and sightly and not significantly reduced IL-6.
| Species | Dose | Route | Cmax | AUC0-∞ |
|---|---|---|---|---|
| Mice[1] | 30 mg/kg | i.g. | 3.2 μM | 3.8 μM·h |
Treatment with S217879 (30 mg/kg; p.o.; once daily; for 8 weeks) significantly ameliorates established non-alcoholic steatohepatitis (NASH) and reduces hepatic fibrosis in diet-induced obese (DIO) mice with NASH[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J mice (8-week-old male; MCDD-induced NASH model)[1]
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Dosage:3 mg/kg/day; 30 mg/kg/day
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Administration:p.o.; daily; 2 weeks
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Result:Reduced NAFLD activity score (NAS) in a dose-dependent manner.
Reduced steatosis and lobular inflammation scores at 30 mg/kg/day.
Increased liver Nqo1 mRNA levels (NRF2 target engagement biomarker) in a dose-dependent manner.
Reduced liver triglycerides in a dose-dependent manner.
Caused a small but significant increase in liver weight.
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Animal Model:C57BL/6JRj mice (5-6-week-old male; aged to 38-39 weeks at termination; AMLN diet-induced NASH with fibrosis model, pre-treatment confirmed fibrosis stage >1 and steatosis score ≥2)[1]
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Dosage:30 mg/kg
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Administration:p.o.; daily; 8 weeks
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Result:Reduced plasma alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels significantly.
Reduced liver triglyceride levels.
Reduced NAS significantly due to decreased lobular inflammation.
Decreased liver galectin-3 staining significantly.
Markedly reduced liver fibrosis, shown by decreased Picrosirius red (PSR) staining, reduced liver hydroxyproline content, reduced collagen 1A1 (Col1A1)-positive area, and reduced alpha smooth muscle actin (αSMA)-positive area.
Chemical Information
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CAS No. 2700303-28-0
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Masse moléculaire 592.66
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Formule C30H32N4O7S
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SMILES
CC1=CC=C(C=C1[C@H](N2C3)C)[C@H](CC(O)=O)C4=CC=C5C(N=NN5CCOCCOC6=CC3=C(OS2(=O)=O)C=C6)=C4C
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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
[1]. Seedorf K, et al. Selective disruption of NRF2-KEAP1 interaction leads to NASH resolution and reduction of liver fibrosis in mice. JHEP Rep. 2022;5(4):100651. Published 2022 Dec 16. [Content Brief]
[2]. Wang Y, et al. cGAS-STING Targeting Offers Novel Therapeutic Opportunities in Liver Diseases. Drug Des Devel Ther. 2025;19:5835-5853. Published 2025 Jul 9. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
S217879 Related Classifications
HY-156065 Related Classifications
Powered by Bioz
- S217879
- 2700303-28-0
- S 217879
- S-217879
- Keap1-Nrf2
- Reactive Oxygen Species (ROS)
- Interleukin Related
- reactive oxygen species
- rodents
- KEAP1-NRF2 protein-protein interaction
- STING
- non-alcoholic steatohepatitis
- apoptosis
- primary human peripheral blood mononuclear cells
- NRF2
- hepatic stellate cells
- DNA damage
- Inhibitor
- inhibitor
- inhibit