R079
R079 (compound 17) is a selective, orally active Nrf2 activator. R079 increases Nrf2 translocation activity (EC50 = 32.41 μM). R079 can neutralize excess levels of reactive oxygen species through activating Nrf2. R079 has anti-inflammatory properties and can be used in multiple sclerosis research .
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- No. CAS: 2115659-62-4
- Fòrmula: C11H11N3O3S
- Peso molecular:265.29
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| THP-1 | IC50 |
3.49 μM
Compound: 17
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Inhibition of LPS-induced IL-23 production in IFN-gamma primed human THP-1 cells preincubated for 1 hr followed by LPS stimulation for 18 hrs by sandwich ELISA
Inhibition of LPS-induced IL-23 production in IFN-gamma primed human THP-1 cells preincubated for 1 hr followed by LPS stimulation for 18 hrs by sandwich ELISA
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[PMID: 38116420] |
PK Parameters for R079 in Balb/c Mice[1]
| Parameter | Balb/c Mice (p.o., 5mg/kg) |
| clearance (mL/min/kg) | 2.01 |
| half-life (h) | 1.0 |
| Vss (L/kg) | 0.14 |
| oral AUC (ng·h/mL) | 22900 |
| oral Cmax (ng/mL) | 19600 (73.96 μM) |
| bioavailability (%F) | 56 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:mouse experimental autoimmune encephalomyelitis (EAE) model[1]
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Dosage:30, 60, and 90 mg/kg
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Administration:Oral gavage (p.o.), b.i.d for 28 days
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Result:Demonstrated a robust dose-dependent reduction in disease severity (41% reduction in clinical score at 30 mg/kg to 89% at 60 mg/kg), p.o. (60, 90 mg/kg) increased levels of Nrf2 for an 8 h period in mouse thymus.
Chemical Information
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No. CAS 2115659-62-4
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Peso molecular 265.29
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Fòrmula C11H11N3O3S
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SMILES
O=S(/C=C/N1C(N(C=N1)C)=O)(C2=CC=CC=C2)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
R079 Related Classifications
HY-163027 Related Classifications
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