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别名 TP-235, RTA-403, CDDO-Imidazolide
CDDO-Im (TP-235) 是一种 Nrf2和 PPAR 的激活剂,对 PPARα 和 PPARγ 的 Ki 分别为232 nM 和 344 nM。


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CDDO-Im (TP-235) 是一种 Nrf2和 PPAR 的激活剂,对 PPARα 和 PPARγ 的 Ki 分别为232 nM 和 344 nM。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 1 mg | ¥ 297 | 现货 | |
| 5 mg | ¥ 597 | 现货 | |
| 10 mg | ¥ 928 | 现货 | |
| 25 mg | ¥ 1,620 | 现货 | |
| 50 mg | ¥ 2,620 | 现货 | |
| 100 mg | ¥ 3,970 | 现货 | |
| 500 mg | ¥ 8,630 | 现货 | |
| 1 mL x 10 mM (in DMSO) | ¥ 712 | 现货 |
CDDO-Im 相关产品
| 产品描述 | CDDO-Im (TP-235) is an activator of Nrf2 and PPAR (Kis: 232/344 nM for PPARα/PPARγ). |
| 靶点活性 | PPARγ:344 nM (Ki), PPARα:232 nM (Ki) |
| 体外活性 | CDDO-Im在抑制人类白血病和乳腺癌细胞系的细胞增殖方面具有高活性(IC50约为10-30 nM)。在U937白血病细胞中,通过增加CD11b和CD36细胞表面表达来衡量,CDDO-Im还诱导单核细胞分化[1]。CDDO-Im处理在三阴性乳腺癌细胞系SUM159和MDA-MB-231中明显诱导细胞周期在G2/M期停滞和凋亡。在SUM159肿瘤球中的CD24^-/EpCAM^+细胞显著被CDDO-Im处理抑制。CDDO-Im还显著降低了初级和二级球体培养中的球体形成效率和肿瘤球大小[2]。用CDDO-Im处理能提高Nrf2蛋白水平,Nrf2是一种先前显示能结合ARE序列并增加Nrf2调控的多种抗氧化和解毒基因表达的转录因子[3]。 |
| 体内活性 | CDDO-Im 对初级小鼠巨噬细胞中新生可诱导型一氧化氮合酶(iNOS)表达具有显著的抑制作用。此外,CDDO-Im 在体内抑制B16小鼠黑色素瘤和L1210小鼠白血病细胞的生长。CDDO-Im 10 nM(5.4 μg)的注射几乎完全阻止了IFN-γ诱导iNOS的能力,而使用少至1 nmol的CDDO-Im(0.54 μg)治疗也具有部分效果[1]。 |
| 细胞实验 | CDDO-Im is dissolved in DMSO. SUM159 and MDA-MB-231 cells are seeded into each well of 96-well plates (1,000 cell/well) and treated the next day with vehicle control or CDDO-Im (1, 10, 50, 100 and 200 nM) for given incubation time. The absorbance is measured with a spectrophotometer to determine the cell proliferation rate [2]. |
| 动物实验 | Mice are injected i.p. with thioglycollate, and the resulting resident peritoneal macrophages are activated 3 days later with an i.p. injection of IFN-γ. CDDO and CDDO-Im are injected i.p. 30 min after IFN-γ. Macrophages are harvested 10 h later, cultured for 12 h, and then assayed for expression of iNOS protein and production of nitric oxide (NO) [1]. |
| 别名 | TP-235, RTA-403, CDDO-Imidazolide |
| 分子量 | 541.72 |
| 分子式 | C34H43N3O3 |
| CAS No. | 443104-02-7 |
| Smiles | [H][C@@]12CC(C)(C)CC[C@@]1(CC[C@]1(C)[C@]2([H])C(=O)C=C2[C@@]1(C)CC[C@@]1([H])C(C)(C)C(=O)C(=C[C@]21C)C#N)C(=O)n1ccnc1 |
| 密度 | 1.23 g/cm3 (Predicted) |
| 颜色 | White |
| 物理性状 | Solid |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| 溶解度信息 | DMSO: 40 mg/mL (73.84 mM), Sonication is recommended. H2O: Insoluble | ||||||||||||||||||||||||||||||
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