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Bardoxolone Methyl

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产品编号 T6165Cas号 218600-53-4
别名 甲基巴多索隆, TP-155, RTA 402, NSC 713200, CDDO Methyl ester

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。

Bardoxolone Methyl
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Bardoxolone Methyl

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纯度: 99.09%
产品编号 T6165 别名 甲基巴多索隆, TP-155, RTA 402, NSC 713200, CDDO Methyl esterCas号 218600-53-4

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。

规格价格库存数量
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 x 10 mM (in DMSO)¥ 452现货
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纯度:99.09%
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产品介绍

生物活性
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)
别名甲基巴多索隆, TP-155, RTA 402, NSC 713200, CDDO Methyl ester
化学信息
分子量505.69
分子式C32H43NO4
CAS No.218600-53-4
Smiles[H][C@@]12CC(C)(C)CC[C@@]1(CC[C@]1(C)C2C(=O)C=C2[C@@]1(C)CC[C@@]1([H])C(C)(C)C(=O)C(=C[C@]21C)C#N)C(=O)OC
密度1.15g/cm3
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 18.33 mg/mL (36.25 mM)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
溶液配制表
1mg5mg10mg50mg
1 mM1.9775 mL9.8875 mL19.7750 mL98.8748 mL
5 mM0.3955 mL1.9775 mL3.9550 mL19.7750 mL
10 mM0.1977 mL0.9887 mL1.9775 mL9.8875 mL
20 mM0.0989 mL0.4944 mL0.9887 mL4.9437 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

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:
TargetMol | Animal experiments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 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent 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 μLDMSOTargetMol | reagent ( 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:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
mg/kg
g
μL
2 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
%
%Tween 80
%ddH2O

剂量转换

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