| Bioactivity | 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]. |
| Invitro | R079 (2-10 μM) 可增加 THP-1 细胞 Nrf2 和 HO-1 的表达[1]。R079 在小鼠、大鼠、狗、猴和人微粒体中具有微粒体稳定性，t1/2大于 60 分钟 [1]。 0 --> R079 相关抗体: |
| In Vivo | R079 (30-90 mg/kg, p.o., b.i.d 28 天) 在小鼠 EAE 模型中显示出稳健且剂量依赖性的疾病严重程度降低[1]。1.19R079 在 Balb/c 鼠体内的药动学参数[1]Parameter |
| Name | R079 |
| CAS | 2115659-62-4 |
| Formula | C11H11N3O3S |
| Molar Mass | 265.29 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |