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R079 (compound 17), a selective and orally active Nrf2 activator, enhances Nrf2 translocation activity (EC 50 = 32.41 μM) and can neutralize excess levels of reactive oxygen species by activating Nrf2. Additionally, R079 possesses anti-inflammatory properties and has applications in multiple sclerosis research [1].
R079 (compound 17), a selective and orally active Nrf2 activator, enhances Nrf2 translocation activity (EC 50 = 32.41 μM) and can neutralize excess levels of reactive oxygen species by activating Nrf2. Additionally, R079 possesses anti-inflammatory properties and has applications in multiple sclerosis research [1].
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
10 mg | 询价 | 10-14周 | |
50 mg | 询价 | 10-14周 |
产品描述 | R079 (compound 17), a selective and orally active Nrf2 activator, enhances Nrf2 translocation activity (EC 50 = 32.41 μM) and can neutralize excess levels of reactive oxygen species by activating Nrf2. Additionally, R079 possesses anti-inflammatory properties and has applications in multiple sclerosis research [1]. |
体内活性 | R079通过每日两次口服投给(30、60、90 mg/kg,这28天),在小鼠实验性自身免疫性脑炎(EAE)模型中显著降低了疾病的严重性,并呈剂量依赖性,其中在60 mg/kg剂量时疾病严重度降低了89% [1]。此外,R079在60, 90 mg/kg剂量下能在小鼠胸腺中提升Nrf2水平持续8小时。药动学研究显示,R079在Balb/c鼠中的清除率为2.01 mL/min/kg,半衰期为1.0小时,稳态分布容积为0.14 L/kg,口服AUC为22900 ng·h/mL,口服C max为19600 ng/mL(73.96 μM),生物利用度为56% [1]。 |
分子量 | 265.29 |
分子式 | C11H11N3O3S |
CAS No. | 2115659-62-4 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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