1. NF-κB
  2. Keap1-Nrf2
  3. 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 .

For research use only. We do not sell to patients.

R079 Chemical Structure

R079 Chemical Structure

CAS No. : 2115659-62-4

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Description

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 [1].

In Vitro

R079 (2-10 μM) increases expression of Nrf2 and HO-1 in THP-1 cells[1].
R079 shows microsomal stability, with t1/2s of >60 min in mouse, rat, dog, monkey and human microsomes [1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

R079 (30-90 mg/kg, p.o., b.i.d for 28 days) demonstrates a robust dose-dependent reduction in disease severity in mouse EAE model[1].
1.19
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.

Animal Model: mouse experimental autoimmune encephalomyelitis (EAE) model[1]
Dosage: 30, 60, and 90 mg/kg
Administration: Oral gavage (p.o.), b.i.d for 28 days
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.
Molecular Weight

265.29

Formula

C11H11N3O3S

CAS No.
SMILES

O=S(/C=C/N1C(N(C=N1)C)=O)(C2=CC=CC=C2)=O

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

Purity & Documentation
References
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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.

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Product Name:
R079
Cat. No.:
HY-163027
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