2. NF-κB Metabolic Enzyme/Protease Immunology/Inflammation
  3. Keap1-Nrf2 Reactive Oxygen Species (ROS) Interleukin Related
  4. 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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S217879

S217879 Chemical Structure

CAS No. : 2700303-28-0

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S217879 Related Antibodies

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Description

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[1][2].

In Vitro

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.

S217879 Related Antibodies

ELISA Assay[1]

Cell Line: PBMCs treated LPS (HY-D1056)
Concentration: 30,100, 300, 1000 nM
Incubation Time: 4 h pre-incubation
Result: Significantly inhibited LPS-induced IL-1β and MCP-1 secretion, and sightly and not significantly reduced IL-6.
Parmacokinetics
Species Dose Route Cmax AUC0-∞
Mice[1] 30 mg/kg i.g. 3.2 μM 3.8 μM·h
In Vivo

S217879 (3-30 mg/kg/day; oral administration; daily dosing; for 2 consecutive weeks) dose-dependently slows the progression of NASH in MCDD-fed mice, significantly reduces NAS and hepatic triglyceride levels, and enhances the binding activity of NRF2 targets[1].
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.

Animal Model: C57BL/6J mice (8-week-old male; MCDD-induced NASH model)[1]
Dosage: 3 mg/kg/day; 30 mg/kg/day
Administration: p.o.; daily; 2 weeks
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.
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]
Dosage: 30 mg/kg
Administration: p.o.; daily; 8 weeks
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.
Molecular Weight

592.66

Formula

C30H32N4O7S
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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S217879 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:

S2178792700303-28-0S 217879S-217879Keap1-Nrf2Reactive Oxygen Species (ROS)Interleukin RelatedILreactive oxygen speciesrodentsKEAP1-NRF2 protein-protein interactionSTINGnon-alcoholic steatohepatitisapoptosisprimary human peripheral blood mononuclear cellsNRF2hepatic stellate cellsDNA damageInhibitorinhibitorinhibit

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