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932730-51-3

中文名称 CS-1305
英文名称 CDDO-EA
CAS 932730-51-3
分子式 C33H46N2O3
分子量 518.73
MOL 文件 932730-51-3.mol
更新日期 2024/07/04 17:30:42
932730-51-3 结构式 932730-51-3 结构式

基本信息

中文别名
NF-E2相关因子2/抗氧化反应元件(NRF2/ARE)激活剂(CDDO-EA)
英文别名
TP319
TP 319
RTA405
TP-319)
CDDO-EA
RTA 405
RTA-405
CS-1305
CDDO ethyl amide
Bardoxolone ethyl amide
所属类别
生物化工:激动剂抑制剂

物理化学性质

沸点670.7±55.0 °C(Predicted)
密度1.13±0.1 g/cm3(Predicted)
储存条件-20°C储存
溶解度DMSO: ≥ 34 mg/mL (65.54 mM)
酸度系数(pKa)16.21±0.70(Predicted)
形态粉末
颜色White to off-white

常见问题列表

生物活性
CDDO-EA 是一种 NF-E2 相关因子 2 /抗氧化反应元件 (Nrf2/ARE) 激活剂。
靶点

Nrf2/ARE

体外研究

CDDO-EA potently activates Nrf2/ARE in a cell culture model of ALS and in the G93A SOD1 mouse model of ALS. CDDO-EA is a potent inducer of apoptosis in A549 lung cancer cells, as shown both by PARP cleavage and Annexin staining. CDDO-EA is more potent than CDDO itself as inducers of heme oxygenase-1 (HO-1). In RAW264.7 macrophage-like cells, CDDO-EA is 7-fold more potent than CDDO as suppressors of the ability of IFN-γ to induce iNOS.

体内研究

The survival analysis shows that G93A mice treated with CDDO-EA, compared to G93A littermate controls, lives significantly longer. CDDO-EA treatment increases the life-span by 20.6 days from 124.05±3.7 days to 144.72±8.1 days (16.6%) (p<0.001). In CDDO-EA-treated G93A mice, the age of death is 141.4±5.2 days and the duration from the age of onset to the age of death is 57.6±7.6 days, which means that the age of death from onset is prolonged by 17.5 days (43%).

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