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Bardoxolone

Bardoxolone

产品编号 T2915   CAS 218600-44-3
别名: RTA 401, 齐墩果烷三萜化合物, CDDO

Bardoxolone (CDDO) 是新型核调节因子激活剂。

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Bardoxolone Chemical Structure
Bardoxolone, CAS 218600-44-3
规格 价格/CNY 货期 数量
5 mg ¥ 667 现货
10 mg ¥ 919 现货
25 mg ¥ 1,171 现货
50 mg ¥ 1,633 现货
100 mg ¥ 2,997 现货
1 mL * 10 mM (in DMSO) ¥ 722 现货
产品目录号及名称: Bardoxolone (T2915)
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纯度: 99.19%
纯度: 98.97%
纯度: 97.9%
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天然产物信息
生物活性
化学信息
存储 & 溶解度
参考文献
植物来源
结构类型
产品描述 Bardoxolone (CDDO) is a synthetic oleanane triterpenoid that blocks the cellular synthesis of inducible nitric oxide synthase and inducible COX-2 in INF-γ-activated mouse macrophages with an IC50 value of 0.4 nM. By suppressing reactive oxygen and nitrogen species (ROS/RNS) formation, it promotes the cellular control of ROS/RNS levels that would lead to DNA damage associated with tumorigenesis. In various Y cell lines, Bardoxolone has been shown to specifically inhibit proliferation and induce apoptosis. Mechanism studies revealed that Bardoxolone is a ligand for peroxisome proliferator-activated receptor γ, and also that it induces genes regulated by Nrf2, including heme oxygenase-1 and eotaxin-1, which play a role in antioxidant response element signaling activity.
体外活性 Bardoxolone methyl is a novel synthetic triterpenoid and antioxidant inflammation modulator that potently induces Nrf2 and inhibits NF-κB and Janus-activated kinase/STAT signaling. Bardoxolone methyl has been shown to induce differentiation, inhibit proliferation, and induce apoptosis in cancer cell lines[2].
体内活性 Kidney sections from Bardoxolone methyl-treated monkeys demonstrates decreased megalin protein expression although similar mRNA expression across groups. The visualized decrease in megalin protein expression is confirmed by densitometry analyses, which demonstrated that Bardoxolone methyl administration significantly decreased megalin protein expression in the monkey kidney. Bardoxolone methyl administration does not affect the protein expression of cubilin in the kidney or the mRNA expression of cubilin in the kidney. The creatinine clearance in monkeys administered Bardoxolone methyl significantly differed from that at baseline and in vehicle-treated animals on day 28. After 28 days of Bardoxolone methyl administration, urinary albumin-to-creatinine ratios (UACRs), determined from the 24-hour urine collections, are significantly increased compared with those in animals receiving vehicle. Of note, UACRs decreases 53.3% in vehicle-treated animals and increased 27.9% in Bardoxolone methyl-treated monkeys[3]. Male C57BL/6J mice are administered oral BARD during HFD feeding (HFD/BARD), only fed a high-fat diet (HFD), or fed low-fat diet (LFD) for 21 weeks. Compared with LFD mice, HFD mice have a marked increase in the number of F4/80 crown-like structures (+95%; p<0.001), which is effectively prevented by BARD (−50%; p<0.01). Similarly, the number of F4/80 interstitial macrophages is significantly higher in HFD mice by 98% (p<0.001) compared with LFD mice and by 32% (p<0.01) compared with HFD/BARD mice[4].
别名 RTA 401, 齐墩果烷三萜化合物, CDDO
分子量 491.66
分子式 C31H41NO4
CAS No. 218600-44-3

存储

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

溶解度

DMSO: 100 mg/mL (203.39 mM), sonification is recommended.

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 2.0339 mL 10.1696 mL 20.3393 mL 50.8481 mL
5 mM 0.4068 mL 2.0339 mL 4.0679 mL 10.1696 mL
10 mM 0.2034 mL 1.017 mL 2.0339 mL 5.0848 mL
20 mM 0.1017 mL 0.5085 mL 1.017 mL 2.5424 mL
50 mM 0.0407 mL 0.2034 mL 0.4068 mL 1.017 mL
100 mM 0.0203 mL 0.1017 mL 0.2034 mL 0.5085 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. McCullough PA, et al. Cardiac and renal function in patients with type 2 diabetes who have chronic kidney disease: potential effectsof bardoxolone methyl. Drug Des Devel Ther. 2012;6:141-9. 2. Hong DS, et al. A phase I first-in-human trial of bardoxolone methyl in patients with advanced solid tumors and lymphomas. Clin Cancer Res. 2012 Jun 15;18(12):3396-406. 3. Reisman SA, et al. Bardoxolone Methyl Decreases Megalin and Activates Nrf2 in the Kidney. J Am Soc Nephrol. 2012 Oct;23(10):1663-73. 4. Dinh CH, et al. Bardoxolone Methyl Prevents Mesenteric Fat Deposition and Inflammation in High-Fat Diet Mice. ScientificWorldJournal. 2015;2015:549352.

文献引用

1. Wang J, Xu J, Yang S, et al.SN‐38, an active metabolite of irinotecan, inhibits transcription of nuclear factor erythroid 2‐related factor 2 and enhances drug sensitivity of colorectal cancer cells.Molecular Carcinogenesis.2024
Antroquinonol 2-tert-Butyl-1,4-benzoquinone CDDO-dhTFEA KI696 Astilbin Curcumin Tigloylgomisin H Luteolin

相关化合物库

该产品包含在如下化合物库中:
抗癌药物库 抗癌活性化合物库 抗癌临床化合物库 植物来源化合物库 高通量筛选天然产物库 氧化还原化合物库 经典已知活性库 转录因子库 ReFRAME 相关化合物库 中药抗炎分子库

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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% Tween 80
% 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 218600-44-3 Immunology/Inflammation Others Nrf2 Inhibitor RTA401 RTA 401 齐墩果烷三萜化合物 CDDO inhibit Keap1-Nrf2 RTA-401 inhibitor

 

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