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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 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 |
| 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. |
| [References]
[1] Simon J. Shaw, et al. Tuning the Reactivity of Nuclear Factor Erythroid 2 Related Factor 2 (Nrf2) Activators for Optimal in Vivo Efficacy. ACS Medicinal Chemistry Letters . 2023，Article ASAP. |
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