CDDO-TFEA
| 规格 | 价格 | 货期 | 数量 |
|---|---|---|---|
| 1mg | ¥1323.00 | 10-15工作日发货 | |
| 5mg | ¥4455.00 | 10-15工作日发货 | |
| 10mg | ¥7886.00 | 10-15工作日发货 |
特色产品
- 用于免疫印迹和质谱分析等后续操作
- 适用于30 KDa-130 KDa大小的蛋白
- 可将信号灵敏度提高100倍
- 同时保持稳定的特异性和分辨率
- 提供更高的转录效率并抑制免疫激活
- 使用5-moUTP和Cy5-utp修饰
产品描述
CDDO-trifluoroethyl-amide (CDDO-TFEA), a trifluoroethylamide derivative of CDDO, is an Nrf2/ARE pathway activator [1][2][3].
The NF-E2-related factor-2 (Nrf2)/antioxidant response element (ARE) signaling pathway is an important pathway involved in antioxidant and anti-inflammatory responses. Modulation of the Nrf2/ARE pathway is an attractive therapeutic target for neurodegenerative diseases such as amyotrophic lateral sclerosis (ALS) and Huntington's disease (HD) [2][3].
CDDO-TFEA is an Nrf2/ARE pathway activator. In NSC-34 G93A SOD1 cells, CDDO-TFEA upregulated Nrf2 expression and caused translocation of Nrf2 into the nucleus. CDDO-TFEA also increased the expression of Nrf2/ARE-regulated proteins (NQO-1, HO-1 and Glutathione reductase).
In mice with experimental autoimmune encephalomyelitis (EAE), CDDO-TFEA reduced immune and inflammatory cell populations. CDDO-TFEA also significantly reduced Th1 and Th17 cytokines (IL6, IL17, IFNγ, TNFα and GMCSF) [1]. In ALS mice model, CDDO-TFEA upregulated the expression and resulted in translocation of Nrf2 to the nucleus of neurons in the spinal cord. In G93A SOD1 mice, CDDO-TFEA increased the life-span by 17.6 days [2].
References:
[1]. Pareek TK, Belkadi A, Kesavapany S, et al. Triterpenoid modulation of IL-17 and Nrf-2 expression ameliorates neuroinflammation and promotes remyelination in autoimmune encephalomyelitis. Sci Rep. 2011;1:201.
[2]. Neymotin A, Calingasan NY, Wille E, et al. Neuroprotective effect of Nrf2/ARE activators, CDDO ethylamide and CDDO trifluoroethylamide, in a mouse model of amyotrophic lateral sclerosis. Free Radic Biol Med. 2011 Jul 1;51(1):88-96.
[3]. Stack C, Ho D, Wille E, et al. Triterpenoids CDDO-ethyl amide and CDDO-trifluoroethyl amide improve the behavioral phenotype and brain pathology in a transgenic mouse model of Huntington's disease. Free Radic Biol Med. 2010 Jul 15;49(2):147-58.
产品性质
| 物理外观 | A crystalline solid |
| CAS号 | 932730-52-4 |
| 分子式 | C33H43F3N2O3 |
| 分子量 | 572.7 |
| 化学名称 | 2-cyano-3,12-dioxo-N-(2,2,2-trifluoroethyl)-oleana-1,9(11)-dien-28-amide |
| 溶解度 | ≤5mg/ml in ethanol;5mg/ml in DMSO;5mg/ml in dimethyl formamide |
| SMILES | CC1(CC[C@@]2(CC[C@@](C)([C@@]3(CC[C@]4(C(C)(C(C(C#N)=C[C@@]4(C3=CC5=O)C)=O)C)[H])C)[C@]5([C@@]2(C1)[H])[H])C(NCC(F)(F)F)=O)C |
| 存储条件 | -20°C |
| 运输条件 | 蓝冰 |
产品应用 (实验数据来自文献,APExBIO并未验证,仅供参考)
IC50和靶点
| 生物活性描述 | CDDO-TFEA (RTA 404;TP-500)是 CDDO 的一种三氟乙酰胺衍生物,具有更强的穿越血脑屏障的能力。CDDO 是一种激活剂,可抑制各种细胞的增殖并诱导其分化。CDDO-TFEA 能在各种神经退行性疾病模型中增强 Nrf2 的表达和信号转导,包括模拟多发性硬化症、肌萎缩性脊髓侧索硬化症和亨廷顿氏病的模型。CDDO-TFEA 可诱导和阻断尤文氏肉瘤和神经母细胞瘤细胞系的集落形成,IC 值范围为 85-170 nM。 |



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