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  2. NF-κB Apoptosis
  3. Keap1-Nrf2 Necroptosis
  4. Bardoxolone

Bardoxolone  (Synonyms: 巴多索隆; CDDO; RTA 401)

目錄號(hào): HY-14909 純度: 98.57%
COA 產(chǎn)品使用指南 技術(shù)支持

Bardoxolone (RTA 401; CDDO) 是一種新型的核調(diào)控因子 (NRf-2) 激活劑。Bardoxolone 是一種有效的壞死性凋亡 (necroptosis) 抑制劑，可抑制 Z-VAD-FMK 誘導(dǎo)的壞死性凋亡。Bardoxolone methyl 增強(qiáng)大鼠腎臟抗氧化系統(tǒng)，調(diào)節(jié)炎癥細(xì)胞因子，抑制細(xì)胞凋亡，顯示出對(duì) APAP 誘導(dǎo)的急性腎損傷 (AKI) 的抑制作用和鎮(zhèn)痛作用。此外，Bardoxolone methyl 可降低 Paclitaxel (PAC) 誘導(dǎo)的神經(jīng)元細(xì)胞線粒體損傷。Bardoxolone methyl 有望用于在化療引起的神經(jīng)性疼痛和慢性腎臟疾病的研究。

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Bardoxolone Chemical Structure

Bardoxolone Chemical Structure

CAS No. : 218600-44-3

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥870
In-stock
1 mg ￥363
In-stock
5 mg ￥800
In-stock
10 mg ￥1100
In-stock
50 mg ￥1950
In-stock
100 mg ￥3600
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200 mg   詢價(jià)  
500 mg   詢價(jià)  

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Customer Review

Other Forms of Bardoxolone:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Bardoxolone (RTA 401; CDDO) is a novel nuclear regulatory factor (NRf-2) activator. Bardoxolone is a potent necroptosis inhibitor that inhibits Z-VAD-FMK-induced necroptosis. Bardoxolone methyl enhances the antioxidant system, modulates inflammatory cytokines and inhibits apoptosis in rat kidney, demonstrating inhibition on APAP-induced acute kidney injury (AKI) and analgesic effect. Additionally, Bardoxolone methyl decreases Paclitaxel (PAC) (HY-B0015)-induced mitochondrial damage in neuronal cells. Bardoxolone methyl is promising for the research of chemotherapy-induced neuropathic pain and chronic kidney disease[1][2][3][4].
IC50 & Target

Nrf-2[1]
細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
HT-29 EC50
1.3 μM
Compound: 7; CDDO
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: 7; CDDO
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
0.0004 μM
Compound: 4, CDDO
Antiinflammatory activity in mouse macrophages assessed as inhibition of IFN-gamma-induced nitric oxide production after 48 hrs by Griess method
Antiinflammatory activity in mouse macrophages assessed as inhibition of IFN-gamma-induced nitric oxide production after 48 hrs by Griess method
[PMID: 23837912]
Macrophage IC50
0.5 nM
Compound: CDDO
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]
Macrophage IC50
4.3 nM
Compound: CDDO
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 EC50
0.16 μM
Compound: CDDO
Cytotoxicity against human MCF7 cells assessed as inhibition of cell proliferation after 3 days by radioactive thymidine incorporation assay
Cytotoxicity against human MCF7 cells assessed as inhibition of cell proliferation after 3 days by radioactive thymidine incorporation assay
[PMID: 26177446]
RAW IC50
20 nM
Compound: CDDO
Inhibition of interferon gamma-stimulated NO production in RAW 264.7 cells after 24 hrs
Inhibition of interferon gamma-stimulated NO production in RAW 264.7 cells after 24 hrs
[PMID: 17367124]
RAW264.7 IC50
11 nM
Compound: CDDO, Bardoxolone
Inhibition of NO production in INFgamma-stimulated mouse RAW264.7 cells measured after 24 hrs by Griess reaction method
Inhibition of NO production in INFgamma-stimulated mouse RAW264.7 cells measured after 24 hrs by Griess reaction method
[PMID: 21441026]
RAW264.7 IC50
16.5 nM
Compound: CDDO
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of IFNgamma-stimulated NO production pretreated for 2 hrs before IFNgamma challenge measured after 24 hrs by Griess reaction
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of IFNgamma-stimulated NO production pretreated for 2 hrs before IFNgamma challenge measured after 24 hrs by Griess reaction
[PMID: 22533790]
RAW264.7 IC50
17 nM
Compound: CDDO
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of IFN-gamma induced NO production after 24 hrs by Griess reaction
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of IFN-gamma induced NO production after 24 hrs by Griess reaction
[PMID: 21361338]
RAW264.7 IC50
23 nM
Compound: CDDO
Inhibition of iNOS in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of nitric oxide production after 48 hrs by Griess assay
Inhibition of iNOS in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of nitric oxide production after 48 hrs by Griess assay
[PMID: 25965897]
RAW264.7 IC50
28.3 nM
Compound: CDDO
Antiinflammatory activity against IFN-gamma-stimulated mouse RAW264.7 cells assessed as nitrite accumulation after 24 hrs by Griess reagent method
Antiinflammatory activity against IFN-gamma-stimulated mouse RAW264.7 cells assessed as nitrite accumulation after 24 hrs by Griess reagent method
[PMID: 20188548]
體外研究
(In Vitro)

Bardoxolone methyl (5, 10 mg/kg) 在大鼠腎勻漿中顯著降低 KIM-1、NGAL、TNF-α、TOS、OSI 水平，改善腎小球和小管的惡化，與 NAC (HY-B0215) 效果類似[3]。
Bardoxolone methyl (0.3 和 1 μM, 28 小時(shí)) 減少 PAC 誘導(dǎo)的背根神經(jīng)節(jié) (DRG) 神經(jīng)元細(xì)胞系線粒體損傷，并增加 PAC 處理的 DRG 細(xì)胞中 pNRf2 的強(qiáng)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.
體內(nèi)研究
(In Vivo)

Bardoxolone methyl (5, 10 mg/kg) 在大鼠腎臟中以劑量依賴性的方式降低 Caspase-3 免疫陽性細(xì)胞的百分比[3]。
Bardoxolone methyl (0-10 mg/kg, 腹腔注射, 單次注射) 對(duì)大鼠有鎮(zhèn)痛作用，但無鎮(zhèn)靜作用[4]。
Bardoxolone methyl [10 mg/kg, 腹腔注射, 從第一次注射 PAC (HY-B0015) 后第 21 天后每天注射 2 次] 通過增加大鼠 DRG 中 pNRf2 和 HO-1 來降低 PAC 誘導(dǎo)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

491.66

Formula

C31H41NO4
CAS 號(hào)
性狀

固體

顏色

White to yellow

中文名稱

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 1 year
-20°C 6 months
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : 100 mg/mL (203.39 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 2.0339 mL 10.1696 mL 20.3393 mL
5 mM 0.4068 mL 2.0339 mL 4.0679 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, 1 year; -20°C, 6 months。-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)?個(gè)月內(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；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/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 (5.08 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 (5.08 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。

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 2%。
方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
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: 99.14%

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, 1 year; -20°C, 6 months。-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)?個(gè)月內(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 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 1.0170 mL 2.0339 mL 5.0848 mL
15 mM 0.1356 mL 0.6780 mL 1.3560 mL 3.3899 mL
20 mM 0.1017 mL 0.5085 mL 1.0170 mL 2.5424 mL
25 mM 0.0814 mL 0.4068 mL 0.8136 mL 2.0339 mL
30 mM 0.0678 mL 0.3390 mL 0.6780 mL 1.6949 mL
40 mM 0.0508 mL 0.2542 mL 0.5085 mL 1.2712 mL
50 mM 0.0407 mL 0.2034 mL 0.4068 mL 1.0170 mL
60 mM 0.0339 mL 0.1695 mL 0.3390 mL 0.8475 mL
80 mM 0.0254 mL 0.1271 mL 0.2542 mL 0.6356 mL
100 mM 0.0203 mL 0.1017 mL 0.2034 mL 0.5085 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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產(chǎn)品名稱：
Bardoxolone
目錄號(hào)：
HY-14909
需求量：