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  2. NF-κB Autophagy Apoptosis
  3. Keap1-Nrf2 Autophagy Apoptosis Ferroptosis
  4. Bardoxolone methyl

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

目錄號(hào): HY-13324 純度: 98.92%
COA 產(chǎn)品使用指南

Bardoxolone methyl (NSC 713200; RTA 402; CDDO Methyl ester) 是一種合成的三萜類化合物，具有潛在的抗腫瘤和抗炎活性，作為 Nrf2 通路的激活劑和 NF-κB 途徑的抑制劑。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào)，我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

Bardoxolone methyl Chemical Structure

Bardoxolone methyl Chemical Structure

CAS No. : 218600-53-4

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規(guī)格 價(jià)格 是否有貨 數(shù)量
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 ￥5400
In-stock
1 g   詢價(jià)  
5 g   詢價(jià)  

* Please select Quantity before adding items.

Customer Review

Other Forms of Bardoxolone methyl:

MCE 顧客使用本產(chǎn)品發(fā)表的 28 篇科研文獻(xiàn)

WB

    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.

    • 生物活性

    • 實(shí)驗(yàn)參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    Bardoxolone methyl (NSC 713200; RTA 402; CDDO Methyl ester) is a synthetic triterpenoid compound with potential antineoplastic and anti-inflammatory activities, acting as an activator of the Nrf2 pathway and an inhibitor of the NF-κB pathway.

    IC50 & Target

    Nrf2[1]
    細(xì)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]
    體內(nèi)研究
    (In Vivo)

    Bardoxolone methyl (30 mg/kg, p.o.) decreases renal expression of megalin but not cubilin, increases creatinine clearance and urinary albumin-to-creatinine ratios, and induces Nrf2 cytoprotective targets in cynomolgus monkeys[1]. Bardoxolone methyl induces overall favorable effects on the heart via its improvement in eGFR in both animal models and clinical trials[2].

    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 號(hào)
    性狀

    固體

    顏色

    White to yellow

    中文名稱

    甲基巴多索隆
    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.
    儲(chǔ)存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn)： 

    DMSO 中的溶解度 : 25 mg/mL (49.44 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開(kāi)封的 DMSO)

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)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
    查看完整儲(chǔ)備液配制表

    * 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用。

    • 摩爾計(jì)算器

    • 稀釋計(jì)算器

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

    質(zhì)量
    =
    濃度
    ×
    體積
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動(dòng)物實(shí)驗(yàn)：

    請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

    以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
    ——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
    以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶

    • 方案 一

      請(qǐng)依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (4.94 mM); 澄清溶液

      此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

      生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
    • 方案 二

      請(qǐng)依序添加每種溶劑： 10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (4.94 mM); 澄清溶液

      此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液，此方案實(shí)驗(yàn)周期在半個(gè)月以上的動(dòng)物實(shí)驗(yàn)酌情使用。

      以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL玉米油中，混合均勻。

    以下溶解方案，請(qǐng)直接配制工作液。建議現(xiàn)用現(xiàn)配，在短期內(nèi)盡快用完。 以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比； 如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶。

    • 方案 一

      請(qǐng)依序添加每種溶劑： Corn Oil

      Solubility: 5 mg/mL (9.89 mM); 懸濁液; 超聲助溶

    • 方案 二

      請(qǐng)依序添加每種溶劑： 50% PEG300    50% Saline

      Solubility: 10 mg/mL (19.77 mM); 懸濁液; Need ultrasonic and warming and heat to 40°C

    動(dòng)物溶解方案計(jì)算器
    請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

    給藥劑量

    mg/kg

    動(dòng)物的平均體重

    g

    每只動(dòng)物的給藥體積

    μL

    動(dòng)物數(shù)量

    只
    由于實(shí)驗(yàn)過(guò)程有損耗，建議您多配一只動(dòng)物的量
    請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過(guò) 2%。
    方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購(gòu)。 ，Tween 80，均可在 MCE 網(wǎng)站選購(gòu)。
    計(jì)算結(jié)果
    工作液所需濃度 : mg/mL
    儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
    您所需的儲(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
    動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
    連續(xù)給藥周期超過(guò)半月以上，請(qǐng)謹(jǐn)慎選擇該方案。
    請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
    純度 & 產(chǎn)品資料

    純度: 99.31%

    參考文獻(xiàn)
    Animal Administration
    [1]

    Two separate in-life studies are conducted in cynomolgus monkeys. In one study, cynomolgus monkeys (n=9/gender/dose group) are administered amorphous bardoxolone methyl by oral gavage, using sesame oil as the vehicle, at 5, 30, and 300 mg/kg once daily for 12 months in a GLP environment. Observations for morbidity, mortality, injury, and the availability of food and water are conducted twice daily for all animals. Clinical observations and body weights are conducted and recorded weekly. Weight data are analyzed by calculating the area under the weight versus time curve using the linear trapezoidal method. Blood samples for clinical chemistry evaluations are collected from all animals pretest and from all animals prior to interim (6-month) and terminal (12-month) necropsies. An additional group of monkeys for each dose group are allowed to recover for 4 weeks.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    參考文獻(xiàn)

    完整儲(chǔ)備液配制表

    * 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)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
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      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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    Inquiry Information

    產(chǎn)品名稱：
    Bardoxolone methyl
    目錄號(hào)：
    HY-13324
    需求量：