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/ Bardoxolone methyl

甲基巴多索隆 /Bardoxolone methyl {[allProObj[0].p_purity_real_show]}

货号：A142891 同义名： RTA 402;NSC 713200

Bardoxolone methyl (NSC 713200; RTA 402; CDDO Methyl ester)是一种合成的三萜类化合物，具有潜在的抗肿瘤和抗炎特性。它通过激活Nrf2通路并同时抑制NF-κB通路发挥作用。

Bardoxolone methyl 化学结构 CAS号：218600-53-4
Bardoxolone methyl 化学结构
CAS号：218600-53-4
Bardoxolone methyl 3D分子结构
CAS号：218600-53-4
Bardoxolone methyl 化学结构 CAS号：218600-53-4
Bardoxolone methyl 3D分子结构 CAS号：218600-53-4
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Bardoxolone methyl 纯度/质量文件 产品仅供科研

货号：A142891 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 NF-κB ↓ 其他靶点 纯度
PDTC ammonium ✔ 98%
QNZ ++++

NF-κB, IC50: 11 nM

 		99%+
Sodium 4-Aminosalicylate Dihydrate ✔ 98%
Sodium Salicylate ✔ 95%
Parthenolide ✔ p53 97% HPLC
JSH-23 +

NF-κB, IC50: 7.1 μM

 		98%
Phenethyl caffeate ✔ 98%
Andrographolide ✔ 98+%
Curcumin ✔ HDAC,Nrf2 98%
SC75741 +++

NF-κB, EC50: 200 nM

 		99%+
CBL0137 HCl ++

NF-κB, EC50: 0.47 μM

 		p53 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Bardoxolone methyl 生物活性

描述 The NF-kB pathway plays a key role in multiple cellular processes, including immune signaling, inflammation, development, proliferation and survival. NF-κB suppression occurred through inhibition, activation, phosphorylation and degradation of IκB-α, p65 phosphorylation, p65 nuclear translocation, and NF-κB-mediated reporter gene transcription. Bardoxolone Methyl is a synthetic triterpenoid based on naturally occurring ursolic and oleanolic acids and can inhibit both constitutive and inducible NF-κB through inhibition of IκB-α kinase. Pre-treatment with 1μM Bardoxolone Methyl for 8h could inhibit TNF-induced IκB-α activation, IκB-α phosphorylation within 30 minutes, and subsequently p65 phosphorylation and p65 nuclear translocation in KBM-5cells, without direct effect on IKK. Consistent with this, as the expression of COX-2, MMP-9 and VEGF is regulated by NF-κB, 1μM Bardoxolone Methyl could inhibit TNF-induced expression of this three proteins in a time-dependent manner in KBM-5 cells pre-treated with Bardoxolone Methyl for 8h. Bardoxolone Methyl could enhance the apoptosis induced by TNF or chemotherapeutic agents, including Taxol, 5-fluorouracil and doxorubicin, through inhibition of NF-κB activation in KBM-5 cells. Oral administration of 10 mg/kg Bardoxolone Methyl for 21 weeks could prevent the colon inflammation induced by high fat diet in mice through its effect on regulation of macrophages, NF-κB, cytokines, Cox2 and Ki67, fat deposition and microflora.
体内研究

Bardoxolone methyl (30 mg/kg, oral administration) reduces renal megalin expression while maintaining cubilin levels, enhances creatinine clearance, reduces urinary albumin-to-creatinine ratios, and activates Nrf2 cytoprotective pathways in cynomolgus monkeys[1].

Bardoxolone methyl elicits beneficial cardiac effects by enhancing estimated glomerular filtration rate (eGFR) in both preclinical studies and clinical trials[2].

Bardoxolone methyl 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
C57BL/6 mouse BMDM cells Cytotoxic assay 24 h Cytotoxicity against C57BL/6 mouse BMDM cells assessed as LDH release after 24 hrs 22533790
human CCD-841-CoN cells Proliferation assay 72 h Antiproliferative activity against human CCD-841-CoN cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, IC50=0.316 μM 25675144
human HCT8 cells Proliferation assay 72 h Antiproliferative activity against human HCT8 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, IC50=0.399 μM 25675144
human HCT8 cells 1 μM Function assay 24 h Inhibition of ERK protein phosphorylation in human HCT8 cells at 1 uM incubated for 24 hrs by Western blotting method 25675144

Bardoxolone methyl 动物研究

Dose Mice[3] (i.p.): min = 1.25 mg/kg, max = 10 mg/kg
Monkeys[4] (p.o.): 30 mg/kg
Administration i.p., p.o.

Bardoxolone methyl 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01500798 Chronic Kidney Disease ... 展开 >> Type 2 Diabetes 收起 << Phase 1 Terminated(IDMC recommendation... 展开 >> for safety concerns) 收起 << - -
NCT01576887 End-Stage Renal Disease ... 展开 >> Type 2 Diabetes Mellitus 收起 << Phase 2 Withdrawn(IDMC recommendation ... 展开 >>for safety concerns) 收起 << October 2013 -
NCT00529113 Pancreatic Neoplasms ... 展开 >> Pancreatic Cancer 收起 << Phase 1 Phase 2 Terminated(To pursue other ind... 展开 >>ications) 收起 << - United States, Colorado ... 展开 >> Rocky Mountain Cancer Center (US Oncology) Denver, Colorado, United States United States, Florida Cancer Centers of Florida (US Oncology) Ocoee, Florida, United States United States, Indiana Central Indiana Cancer Centers (US Oncology) Indianapolis, Indiana, United States United States, Texas Sammons Cancer Center (US Oncology) Dallas, Texas, United States, 75246 United States, Washington Northwest Cancer Specialist- Vancouver Cancer Specialist (US Oncology) Vancouver, Washington, United States 收起 <<

Bardoxolone methyl 参考文献

[1]Reisman SA, et al. Bardoxolone Methyl Decreases Megalin and Activates Nrf2 in the Kidney. J Am Soc Nephrol. 2012 Aug 2.

[2]McCullough PA, et al. Cardiac and renal function in patients with type 2 diabetes who have chronic kidney disease: potential effects of bardoxolone methyl. Drug Des Devel Ther. 2012;6:141-9.

Bardoxolone methyl 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.98mL

0.40mL

0.20mL

9.89mL

1.98mL

0.99mL

19.77mL

3.96mL

1.98mL

Bardoxolone methyl 技术信息

CAS号218600-53-4
分子式C32H43NO4
分子量 505.688
别名 RTA 402;NSC 713200;CDDO-Me;TP-155;CDDO Methyl ester
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Store in freezer, under -20°C
溶解度

DMSO: 25 mg/mL(49.44 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

4%DMSO+30% PEG300+5% Tween+61%water 2.5 mg/mL

Tags: Bardoxolone methyl | RTA 402;NSC 713200;CDDO-Me;TP-155;CDDO Methyl ester | NF-κB | IKK | AmBeed-信号通路专用抑制剂 | Bardoxolone methyl 纯度/质量文件 | Bardoxolone methyl 亚型比较 | Bardoxolone methyl 生物活性 | Bardoxolone methyl 细胞研究 | Bardoxolone methyl 动物研究 | Bardoxolone methyl 临床数据 | Bardoxolone methyl 参考文献 | Bardoxolone methyl 实验方案 | Bardoxolone methyl 技术信息

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