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Bardoxolone Methyl

Bardoxolone Methyl

产品编号 T6165   CAS 218600-53-4
别名: RTA 402, CDDO Methyl ester, TP-155, 甲基巴多索隆, NSC 713200

Bardoxolone Methyl (TP-155) 是一种合成的三萜类化合物,作为 Nrf2通路的激活剂和 NF-κB 途径的抑制剂,具有潜在的抗肿瘤和抗炎活性。

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Bardoxolone Methyl Chemical Structure
Bardoxolone Methyl, CAS 218600-53-4
规格 价格/CNY 货期 数量
5 mg ¥ 257 现货
10 mg ¥ 398 现货
25 mg ¥ 637 现货
50 mg ¥ 828 现货
100 mg ¥ 1,230 现货
200 mg ¥ 1,980 现货
500 mg ¥ 3,370 现货
1 mL * 10 mM (in DMSO) ¥ 452 现货
产品目录号及名称: Bardoxolone Methyl (T6165)
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纯度: 99.09%
纯度: 98.94%
纯度: 97.81%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Bardoxolone Methyl (TP-155) is a synthetic triterpenoid that acts as an activator of the Nrf2 pathway and an inhibitor of the NF-κB pathway with potential anti-tumor and anti-inflammatory activities.
体外活性 Bardoxolone Methyl exhibits potent inhibitory activities against production of nitric oxide induced by interferon-? in mouse macrophages with IC50 of 0.1 nM. [1] Bardoxolone Methyl decreases the viability of leukemic HL-60, KG-1, and NB4 cells with IC50 of 0.4, 0.4, and 0.27 μM, respectively. CDDO-Me induces pro-apoptotic Bax protein, inhibits the activation of ERK1/2, and it blocks Bcl-2 phosphorylation, which contributes to the induction of apoptosis. [2] Bardoxolone Methyl potently inhibits both constitutive and inducible NF-kappaB activated by TNF, interleukin (IL)-1beta, phorbol ester, okadaic acid, hydrogen peroxide, lipopolysaccharide, and cigarette smoke. [3]
体内活性 Bardoxolone Methyl (60 mg/kg) reduces the number, size, and severity of lung tumors in vivo. [4] Bardoxolone Methyl significantly reduces the in vivo inflammatory cytokine response following LPS challenge, induces HO-1 protein expression in the spleen, and protects mice against lethal-dose LPS. [5]
激酶实验 IKK assay : To determine the effect of CDDO-Me on TNF-induced IKK activation, IKK is analyzed. Briefly, the IKK complex from whole-cell extracts was precipitated with antibody against IKKα and IKKβ and then treated with protein A/G-Sepharose beads. After 2 hours, the beads are washed with lysis buffer and then resuspended in a kinase assay mixture containing 50 mmol/L HEPES (pH 7.4), 20 mmol/L MgCl2, 2 mmol/L DTT, 20 μCi [γ-32P]ATP, 10 μmol/L unlabeled ATP, and 2 μg of substrate glutathione S-transferase-IκBα (amino acids 1-54). After incubation at 30°C for 30 minutes, the reaction is terminated by boiling with SDS sample buffer for 5 minutes. Finally, the protein is resolved on 10% SDS-PAGE, the gel is dried, and the radioactive bands are visualized with a Storm820. To determine the total amounts of IKK-α and IKK-β in each sample, 50 μg of whole-cell proteins are resolved on 7.5% SDS-PAGE, electrotransferred to a nitrocellulose membrane, and then blotted with either anti-IKK-α or anti-IKK-β antibody.
细胞实验 Leukemic cell lines are cultured at a density of 3.0 × 105 cells/mL, and AML mononuclear cells are cultured at 5 × 105 cells/mL in the presence or absence of indicated concentrations of CDDO-Me. Appropriate amounts of DMSO (final concentration less than 0.05%) are included as control. For cytotoxicity studies, 1 μM ara-C is added to the cultures. After 24 to 72 hours, viable cells are counted with the trypan blue dye exclusion method using a hematocytometer. (Only for Reference)
别名 RTA 402, CDDO Methyl ester, TP-155, 甲基巴多索隆, NSC 713200
分子量 505.69
分子式 C32H43NO4
CAS No. 218600-53-4

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 20 mg/mL (39.5 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9775 mL 9.8875 mL 19.775 mL 49.4374 mL
5 mM 0.3955 mL 1.9775 mL 3.955 mL 9.8875 mL
10 mM 0.1977 mL 0.9887 mL 1.9775 mL 4.9437 mL
20 mM 0.0989 mL 0.4944 mL 0.9887 mL 2.4719 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Honda T, et al. J Med Chem. 2000, 43(22), 4233-4246. 2. Konopleva M, et al. Blood. 2002, 99(1), 326-335. 3. Shishodia S, et al. Clin Cancer Res. 2006, 12(6), 1828-1838. 4. Liby K, et al. Cancer Res. 2007, 67(6), 2414-2419. 5. Auletta JJ, et al. J Interferon Cytokine Res. 2010, 30(7), 497-508.
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相关化合物库

该产品包含在如下化合物库中:
抗癌活性化合物库 抗癌药物库 抗癌上市药物库 抗癌临床化合物库 儿童药物库 FDA 上市激酶抑制剂库 细胞焦亡化合物库 免疫/炎症分子化合物库 抗癌化合物库 细胞凋亡化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

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。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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% ddH2O
计算 重置

技术支持

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。

Keywords

Bardoxolone Methyl 218600-53-4 Apoptosis Autophagy Immunology/Inflammation NF-Κb Ferroptosis IκB/IKK Nrf2 RTA 402 CDDO Methyl ester TP155 inhibit Keap1-Nrf2 Inhibitor NSC713200 RTA-402 RTA402 TP-155 甲基巴多索隆 NSC 713200 TP 155 NSC-713200 inhibitor

 

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