2. NF-κB
  3. Keap1-Nrf2
  4. R079

R079 (化合物 17) 是一种具有选择性、口服活性的 Nrf2 激活剂。R079 增加 Nrf2 转位活性 (EC50 = 32.41 μM)。R079 可通过激活 Nrf2 来中和过量的活性氧物质水平。R079 具有抗炎性质并且可用于多发性硬化研究。

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R079 Chemical Structure

R079 Chemical Structure

CAS No. : 2115659-62-4

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R079 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(In Vitro)

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]。

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

R079 相关抗体:
体内研究
(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]。
1.19
R079 在 Balb/c 鼠体内的药动学参数[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

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.
分子量

265.29

Formula

C11H11N3O3S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

R079 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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.

Keywords:

R0792115659-62-4R 079R-079Keap1-Nrf2Nrf2 ActivatorElectrophilicityMultiple sclerosisNeurological Diseaseanti-inflammatoryBalb/c MiceMouse EAE modelTHP-1 cellInhibitorinhibitorinhibit

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