Bardoxolone methyl (Synonyms: 甲基巴多索隆; RTA 402; NSC 713200; CDDO Methyl ester)

目录号: HY-13324 纯度: 98.92%: Data Sheet SDS COA 产品使用指南
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Bardoxolone (CDDO; RTA 401) methyl 是一种具有口服活性和脑渗透性的 Nrf2 激活剂，也是 SARS-CoV-2 3CL 蛋白酶 (SARS-CoV-2 3CL protease) 的抑制剂。Bardoxolone methyl 在 Vero 细胞中抑制 SARS-CoV-2 复制，EC₅₀ 值为 0.29 μM。Bardoxolone methyl 能提高 pNrf2 和 HO-1 的水平，抑制如 pNFκB 和 MCP-1 等炎症介质。Bardoxolone methyl 通过激活 Nrf2 通路增强抗氧化和抗炎反应，抑制病毒复制，并改善线粒体功能。Bardoxolone methyl 可用于化疗诱导的神经病理性疼痛 (CINP)、COVID-19 以及慢性肾病 (CKD) 的研究。

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Bardoxolone methyl Chemical Structure

CAS No. : 218600-53-4

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥550	In-stock
5 mg	￥312	In-stock
10 mg	￥500	In-stock
50 mg	￥1000	In-stock
100 mg	￥1500	In-stock
200 mg	￥2500	In-stock
500 mg	￥4050	In-stock
1 g		询价
5 g		询价

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Other Forms of Bardoxolone methyl:

Bardoxolone In-stock

MCE 顾客使用本产品发表的 30 篇科研文献

: Bardoxolone methyl purchased from MCE. Usage Cited in: Toxicol Lett. 2016 Sep 30;259:52-59. [Abstract]; MATE1/SCL47A1 efflux transporter expression in hPTCs. Protein (n=3) expression is assessed after administration of NSC 119875 and pre- or delayedexposure to CDDO-Me after 12 h. GAPDH is used as a housekeeping gene. β-actin is used as a loading control.

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生物活性
纯度 & 产品资料
参考文献

生物活性

Bardoxolone (CDDO; RTA 401) methyl is an orally active and brain-penetrant activator of Nrf2 and an inhibitor of SARS-CoV-2 3CL protease. Bardoxolone methyl inhibits SARS-CoV-2 replication in Vero cells with an EC₅₀ value of 0.29 μM. Bardoxolone methyl increases levels of pNrf2 and HO-1, inhibits inflammatory mediators like pNFκB and MCP-1. Bardoxolone methyl activates the Nrf2 pathway to enhance antioxidant and anti-inflammatory responses, inhibits viral replication, and improves mitochondrial function. Bardoxolone methyl can be used in research on chemotherapy-induced neuropathic pain (CINP), COVID-19, and chronic kidney disease (CKD)^[1]^[2]^[3]^[4]^[5].

IC₅₀ & Target

Nrf2^[1]

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.36 μM Compound: CDDO-Me	Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 31051401]
A549	IC₅₀	0.52 μM Compound: CDDO-Me	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 31725288]
A549	IC₅₀	0.63 μM Compound: CDDO-Me	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 35238566]
A549	IC₅₀	2.074 μM Compound: CDDO-Me	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 29501947]
A549/TR	IC₅₀	1.703 μM Compound: CDDO-Me	Antiproliferative activity against human A549/TR cells after 72 hrs by MTT assay Antiproliferative activity against human A549/TR cells after 72 hrs by MTT assay	[PMID: 29501947]
B16-F10	IC₅₀	5.85 μM Compound: CDDO-Me	Cytotoxicity against mouse B16F10 cells after 48 hrs by MTT assay Cytotoxicity against mouse B16F10 cells after 48 hrs by MTT assay	[PMID: 24685545]
CCD-841CoN	IC₅₀	0.316 μM Compound: CDDO-Me	Antiproliferative activity against human CCD-841-CoN cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay Antiproliferative activity against human CCD-841-CoN cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay	[PMID: 25675144]
H9c2	IC₅₀	5.2 μM Compound: CDDO-Me	Cytotoxicity against rat H9c2 cells assessed as reduction in cell viability after 24 hrs by MTT assay Cytotoxicity against rat H9c2 cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 28994286]
HCT-116	IC₅₀	0.25 nM Compound: CDDO-Me	Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay	[PMID: 30429953]
HCT-116	IC₅₀	0.84 μM Compound: CDDO-Me	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 35238566]
HCT-8	IC₅₀	0.29 μM Compound: CDDO-Me	Antiproliferative activity against human HCT8 cells after 72 hrs by SRB assay Antiproliferative activity against human HCT8 cells after 72 hrs by SRB assay	[PMID: 30429953]
HCT-8	IC₅₀	0.363 μM Compound: CDDO-Me	Antiproliferative activity against 5-FU resistant human HCT8 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay Antiproliferative activity against 5-FU resistant human HCT8 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay	[PMID: 25675144]
HCT-8	IC₅₀	0.399 μM Compound: CDDO-Me	Antiproliferative activity against human HCT8 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay Antiproliferative activity against human HCT8 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay	[PMID: 25675144]
HEK293	IC₅₀	2.2 μM Compound: CDDO-Me	Cytotoxicity against HEK293 cells assessed as reduction in cell viability after 24 hrs by MTT assay Cytotoxicity against HEK293 cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 28994286]
HepG2	IC₅₀	0.26 μM Compound: CDDO-Me	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 31051401]
HepG2	IC₅₀	0.52 μM Compound: CDDO-Me	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 31725288]
HepG2	IC₅₀	4.99 μM Compound: CDDO-Me	Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay	[PMID: 24685545]
HOS	IC₅₀	0.66 μM Compound: CDDO-Me	Antiproliferative activity against human HOS cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human HOS cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 31725288]
HT-29	IC₅₀	0.28 μM Compound: CDDO-Me	Antiproliferative activity against human HT-29 cells after 72 hrs by SRB assay Antiproliferative activity against human HT-29 cells after 72 hrs by SRB assay	[PMID: 30429953]
HT-29	EC₅₀	4.34 μM Compound: 10; CDDO-Me	Anti-necroptotic activity in human HT-29 cells assessed as inhibition of TNFalpha/SM-164/Z-VAD-fmk (TSZ)-induced necroptosis by measuring increase in cell viability measured after 12 hrs by celltiter-glo luminescent cell viability assay Anti-necroptotic activity in human HT-29 cells assessed as inhibition of TNFalpha/SM-164/Z-VAD-fmk (TSZ)-induced necroptosis by measuring increase in cell viability measured after 12 hrs by celltiter-glo luminescent cell viability assay	[PMID: 33248849]
L929	EC₅₀	> 10 μM Compound: 10; CDDO-Me	Anti-necroptotic activity in mouse L929 cells assessed as inhibition of TNFalpha/Z-VAD-fmk (TZ)-induced necroptosis by measuring increase in cell viability measured after 12 hrs by celltiter-glo luminescent cell viability assay Anti-necroptotic activity in mouse L929 cells assessed as inhibition of TNFalpha/Z-VAD-fmk (TZ)-induced necroptosis by measuring increase in cell viability measured after 12 hrs by celltiter-glo luminescent cell viability assay	[PMID: 33248849]
Macrophage	IC₅₀	0.2 nM Compound: CDDO-Me	Antiinflammatory activity in CD-1 mouse Macrophage assessed as inhibition of IFN-gamma induced NO production after 48 hrs by Griess reaction Antiinflammatory activity in CD-1 mouse Macrophage assessed as inhibition of IFN-gamma induced NO production after 48 hrs by Griess reaction	[PMID: 21361338]
MCF7	IC₅₀	0.35 μM Compound: CDDO-Me	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 31051401]
MCF7	IC₅₀	0.85 μM Compound: CDDO-Me	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 31725288]
MDA-MB-231	IC₅₀	0.56 μM Compound: CDDO-Me	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 35238566]
U2OS	IC₅₀	0.74 μM Compound: CDDO-Me	Antiproliferative activity against human U2OS cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human U2OS cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 35238566]

体外研究
(In Vitro)

Bardoxolone methyl (5, 10 mg/kg) 在大鼠肾匀浆中显著降低 KIM-1、NGAL、TNF-α、TOS、OSI 水平，改善肾小球和小管的恶化，与 NAC (HY-B0215) 效果类似^[3]。
Bardoxolone methyl (0.3 和 1 μM, 28 小时) 减少 PAC 诱导的背根神经节 (DRG) 神经元细胞系线粒体损伤，并增加 PAC 处理的 DRG 细胞中 pNRf2 的强度^[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Immunofluorescence^[4]

Cell Line:	PAC (10 µM)-treated DRG Cells
Concentration:	0.3 and 1 μM
Incubation Time:	28 h
Result:	Increased pNRf2 intensity in PAC-treated DRG cells.

体内研究
(In Vivo)

Bardoxolone methyl (30 mg/kg, 口服) 可降低食蟹猴肾中巨蛋白的表达，但不影响肾细胞黏附分子的表达，可提高肌酐清除率和尿白蛋白与肌酐比值，并诱导 Nrf2 细胞保护靶点^[1]。
Bardoxolone methyl 通过改善动物模型和临床试验中的估算肾小球滤过率 (eGFR)，对心脏总体产生有利影响^[2]。
Bardoxolone methyl (5, 10 mg/kg) 在大鼠肾脏中以剂量依赖性的方式降低 Caspase-3 免疫阳性细胞的百分比^[3]。
Bardoxolone methyl (0-10 mg/kg, 腹腔注射, 单次注射) 对大鼠有镇痛作用，但无镇静作用^[4]。
Bardoxolone methyl [10 mg/kg, 腹腔注射, 从第一次注射 PAC (HY-B0015) 后第 21 天后每天注射 2 次] 通过增加大鼠 DRG 中 pNRf2 和 HO-1 来降低 PAC 诱导的 pNFκB 和 MCP-1 水平^[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

505.69

Formula

C₃₂H₄₃NO₄

CAS 号

218600-53-4

性状

固体

颜色

White to yellow

中文名称

甲基巴多索隆

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

溶解性数据

细胞实验：

DMSO 中的溶解度 : 25 mg/mL (49.44 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9775 mL	9.8875 mL	19.7750 mL
5 mM	0.3955 mL	1.9775 mL	3.9550 mL
10 mM	0.1977 mL	0.9887 mL	1.9775 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.94 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.94 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
方案三

请依序添加每种溶剂： 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: 2.5 mg/mL (4.94 mM); 悬浊液; 超声助溶

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

方案一

请依序添加每种溶剂： Corn Oil
Solubility: 5 mg/mL (9.89 mM); 悬浊液; 超声助溶
方案二

请依序添加每种溶剂： 50% PEG300 50% Saline
Solubility: 10 mg/mL (19.77 mM); 悬浊液; Need ultrasonic and warming and heat to 40°C

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.31%

选择批次：

Data Sheet (662 KB) SDS (393 KB)

COA (292 KB) HNMR (217 KB) LCMS (120 KB)

产品使用指南 (1538 KB)

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. [Content Brief]

[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. [Content Brief]

[3]. Yasemin Teksen, et al. Bardoxolone methyl attenuates acetaminophen-induced acute kidney injury by suppressing oxidative stress, inflammation and apoptosis[J]. 2024 May 29;31(5):372–379

[4]. Kim HK, et al. Bardoxolone Methyl Ameliorates Chemotherapy-Induced Neuropathic Pain by Activation of Phosphorylated Nuclear Factor Erythroid 2-Related Factor 2 in the Dorsal Root Ganglia. Anesth Analg. 2024 Mar 1;138(3):664-675. [Content Brief]

[5]. Sun Q, et al. Bardoxolone and bardoxolone methyl, two Nrf2 activators in clinical trials, inhibit SARS-CoV-2 replication and its 3C-like protease. Signal Transduct Target Ther. 2021 May 29;6(1):212. [Content Brief]

Bardoxolone methyl 相关分类

Inflammation/Immunology Infection Cardiovascular Disease

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.9775 mL	9.8875 mL	19.7750 mL	49.4374 mL
	5 mM	0.3955 mL	1.9775 mL	3.9550 mL	9.8875 mL
	10 mM	0.1977 mL	0.9887 mL	1.9775 mL	4.9437 mL
	15 mM	0.1318 mL	0.6592 mL	1.3183 mL	3.2958 mL
	20 mM	0.0989 mL	0.4944 mL	0.9887 mL	2.4719 mL
	25 mM	0.0791 mL	0.3955 mL	0.7910 mL	1.9775 mL
	30 mM	0.0659 mL	0.3296 mL	0.6592 mL	1.6479 mL
	40 mM	0.0494 mL	0.2472 mL	0.4944 mL	1.2359 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Bardoxolone methyl (Synonyms: 甲基巴多索隆; RTA 402; NSC 713200; CDDO Methyl ester)

Customer Review

Other Forms of Bardoxolone methyl:

MCE 顾客使用本产品发表的 30 篇科研文献

Bardoxolone methyl 相关产品

•相关化合物库:

•同靶点产品:

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参考文献

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Bardoxolone methyl (Synonyms: 甲基巴多索隆; RTA 402; NSC 713200; CDDO Methyl ester)

Customer Review

Other Forms of Bardoxolone methyl:

Bardoxolone methyl 相关抗体

MCE 顾客使用本产品发表的 30 篇科研文献

Bardoxolone methyl 相关产品

•相关化合物库:

•同靶点产品:

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