Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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/CNY | 货期 | 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 * 10 mM (in DMSO) | ¥ 712 | 现货 |
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 is highly active in suppressing cellular proliferation of human leukemia and breast cancer cell lines (IC50 approximately 10-30 nM). In U937 leukemia cells, CDDO-Im also induces monocytic differentiation as measured by increased cell surface expression of CD11b and CD36 [1]. CDDO-Im treatment markedly induces cell cycle arrest at G2/M-phase and apoptosis in the triple-negative breast cancer cell lines, SUM159 and MDA-MB-231. The CD24?/EpCAM+ cells in SUM159 tumorspheres are significantly inhibited by CDDO-Im treatment. CDDO-Im also significantly decreases sphere-forming efficiency and tumorsphere size in both primary and secondary sphere cultures [2]. Treatment with CDDO-Im elevates protein levels of Nrf2, a transcription factor previously shown to bind ARE sequences and increases expression of a number of antioxidant and detoxification genes regulated by Nrf2 [3]. |
体内活性 | CDDO-Im has potent inhibitory against de novo inducible nitric oxide synthase expression in primary mouse macrophages. Moreover, CDDO-Im inhibits growth of B16 murine melanoma and L1210 murine leukemia cells in vivo. Injection of 10 nM (5.4 μg) of CDDO-Im almost completely blocks the ability of IFN-γ to induce iNOS, and treatment with as little as 1 nmol of CDDO-Im (0.54 μg) is partially effective [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 | RTA-403, CDDO-Imidazolide, TP-235 |
分子量 | 541.72 |
分子式 | C34H43N3O3 |
CAS No. | 443104-02-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (92.30 mM), sonification is recommended.
H2O: Insoluble
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.846 mL | 9.2299 mL | 18.4597 mL | 46.1493 mL |
5 mM | 0.3692 mL | 1.846 mL | 3.6919 mL | 9.2299 mL | |
10 mM | 0.1846 mL | 0.923 mL | 1.846 mL | 4.6149 mL | |
20 mM | 0.0923 mL | 0.4615 mL | 0.923 mL | 2.3075 mL | |
50 mM | 0.0369 mL | 0.1846 mL | 0.3692 mL | 0.923 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
CDDO-Im 443104-02-7 Apoptosis DNA Damage/DNA Repair Immunology/Inflammation Metabolism Others Ferroptosis Nrf2 PPAR inhibit Keap1-Nrf2 RTA 403 CDDO Im Inhibitor TP 235 Peroxisome proliferator-activated receptors RTA-403 RTA403 CDDOIm TP235 CDDO-Imidazolide TP-235 inhibitor