Bardoxolone Methyl

For research use only. Not for use in humans.

目录号:S8078 别名: RTA 402, TP-155, NSC 713200, CDDO Methyl Ester, CDDO-Me

Bardoxolone Methyl Chemical Structure

CAS No. 218600-53-4

Bardoxolone Methyl (RTA 402, TP-155, NSC 713200, CDDO Methyl Ester, CDDO-Me) 是一种IKK抑制剂,具有强的促凋亡和抗炎活性。同时还是有效的Nrf2激活剂和NF-κB抑制剂。Bardoxolone Methyl 可抑制铁死亡。Bardoxolone Methyl 在癌细胞中可诱导凋亡和自噬。

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客户使用Selleck生产的Bardoxolone Methyl发表文献12篇:

客户使用该产品的3个实验数据:

  • Renal Nrf2 activity was shown in RTA402-treated acFSGS (RTA402 + acFSGS) mice as early as day 7 (RTA402 + acFSGS) and persisted to day 28, compared to vehicle + acFSGS mice. Kidney in situ ROS production demonstrated by DHE detection.

    Free Radic Biol Med, 2014, 73:260-9 . Bardoxolone Methyl purchased from Selleck.

    KG-1a cells were treated with Bar (0.5 µM) or a vehicle for 48 h and Annexin V/PI staining was detected after 48 h by flow cytometry.

    Oncol Rep, 2017, 38(3):1517-1524. Bardoxolone Methyl purchased from Selleck.

  • Cells were exposed to increasing concentrations of Bardoxolone methyl (BM; 0–1000 nM) and AR protein levels were measured. Top panels show representative immunoblots depicting AR-FL, AR-V7 and GAPDH levels. Bottom panels show fold change in AR proteins, normalized to GAPDH levels.

    Oncol Rep, 2017, 38(5):2774-2786. Bardoxolone Methyl purchased from Selleck.

产品安全说明书

IκB/IKK抑制剂选择性比较

生物活性

产品描述 Bardoxolone Methyl (RTA 402, TP-155, NSC 713200, CDDO Methyl Ester, CDDO-Me) 是一种IKK抑制剂,具有强的促凋亡和抗炎活性。同时还是有效的Nrf2激活剂和NF-κB抑制剂。Bardoxolone Methyl 可抑制铁死亡。Bardoxolone Methyl 在癌细胞中可诱导凋亡和自噬。
特性 Bardoxolone Methyl是一种口服有效的抗炎症调节剂,唯一用于临床实体瘤,2型糖尿病和慢性肾脏疾病的IKKβ抑制剂。
靶点
IKK [3]
(Cell-free assay)
Ferroptosis [7]
()
Nrf2 [6]
()
NF-κB [6]
()
体外研究

Bardoxolone Methyl作用于小鼠巨噬细胞,对interferon-Ƴ诱导的一氧化氮的产生具有强效的抑制活性,其IC50 为0.1 nM 。[1] Bardoxolone Methyl降低白血病HL-60,KG-1和NB4细胞的生存能力,其IC50分别为 0.4,0.4,和0.27μM。 CDDO-ME诱导促凋亡Bax蛋白表达,抑制ERK1 / 2的活化,并且它抑制Bcl-2的磷酸化,这有助于诱导细胞凋亡。[2] Bardoxolone Methyl可有效地抑制(IL)-1beta, phorbol ester, okadaic acid, hydrogen peroxide, lipopolysaccharide, 和cigarette smoke激活的组成型和可诱导的NF-κB的肿瘤坏死因子。[3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MCF-7 cells MlPvVJJwdGmoZYLheIlwdiCjc4PhfS=> M1TOZmlvcGmkaYTvdpkh[2:wY3XueJJifGmxbjDh[4FqdnO2IIDyc4xq\mW{YYTpc44hd2ZiTVPGMVchMEWUIGDvd4l1cX[nKTDidoVie3RiY3HuZ4VzKGOnbHzzMEBKSzVyPUCuNFUh|ryP NUS1UmF2OTV|NkmzPVY>
human CCD-841-CoN cells NVjJWFh6WHKxbHnm[ZJifGmxbjDhd5NigQ>? M3zkdVczKGh? M1viZ2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQ1PEMVg1OS2Fb16gZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iClZXzsJJBzd2yrZnXyZZRqd25iYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0xNjNzNjFOwG0> MX2yOVY4PTF2NB?=
human HCT8 cells Mn;sVJJwdGmoZYLheIlwdiCjc4PhfS=> NFzKe3A4OiCq M1LhZ2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUPEBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHPlcIwheHKxbHnm[ZJifGmxbjDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTBwM{m5JO69VQ>? NX2wc3JQOjV4N{WxOFQ>
human HepG2 cells M2[3UGN6fG:2b4jpZ:Kh[XO|YYm= MYG0PEBp M1\Gc2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhmeEd{IHPlcIx{KGGodHXyJFQ5KGi{czDifUBOXFRiYYPzZZnwxIxiSVO1NF01Njl7IN88US=> NV73SlNjOjR4OEW1OFU>
mouse B16F10 cells MkDvR5l1d3SxeHnjxsBie3OjeR?= NX\OW|dtPDhiaB?= M12zdWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KG2xdYPlJGIyPkZzMDDj[YxteyCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVUvQDVizszN Ml;SNlQ3QDV3NEW=
C57BL/6 mouse BMDM cells MlvsR5l1d3SxeHnjxsBie3OjeR?= M1;OOFI1KGh? NX7GWIVoS3m2b4TvfIlkcXS7IHHnZYlve3RiQ{W3RmwwPiCvb4Xz[UBDVUSPIHPlcIx{KGG|c3Xzd4VlKGG|IFzETEBz\WynYYPlJIFnfGW{IEK0JIhzew>? NYDTOXF5OjJ3M{O3PVA>
human HCT8 cells M4Xmb2Z2dmO2aX;uJIF{e2G7 MYWxJO69VQ>? NF21OYQzPCCq NGDBVmhKdmirYnn0bY9vKG:oIFXST{Bxem:2ZXnuJJBpd3OyaH;yfYxifGmxbjDpckBpfW2jbjDIR3Q5KGOnbHzzJIF1KDFidV2gbY5kfWKjdHXkJIZweiB{NDDodpMh[nliV3XzeIVzdiCkbH;0eIlv\yCvZYToc4Q> Mn7DNlU3PzVzNES=
mouse PANC1343 cells NVTiUYZNWHKxbHnm[ZJifGmxbjDhd5NigQ>? NX;IZ49QOzByIITvJFExODBibl2= MUO3NkBp M{nkeGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgcY92e2ViUFHOR|E{PDNiY3XscJMh[XRiM{CwJJRwKDFyMECgcm0h[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfS=> MXGyOFM5QDhyNh?=
mouse RAW264.7 cells MmS1SpVv[3Srb36gZZN{[Xl? M3\aOlExOCCwTR?= M1TlSFE5KGh? M2DRTWFvfGmxeHnkZY51KGGldHn2bZR6KGmwIH3veZNmKFKDV{K2OE44KGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[geGJJWC2rbnT1Z4VlKFKRUzDwdo9lfWO2aX;uJIF1KDFyMDDuUUBxemW2cnXheIVlKG[xcjCxPEBpenNiYnXmc5JmKGOqYXzs[Y5o\SCvZXHzeZJm\CCjZoTldkAyPSCvaX7zJIJ6KEh{RFPGRU1j[XOnZDDmcI94KGO7dH;t[ZRzgQ>? NX[5[Gd4OjR|OEi4NFY>
mouse PANC1343 cells Mlr2VJJwdGmoZYLheIlwdiCjc4PhfS=> M1vDZVMxOCC2bzCxNFAxKG6P NF3kU484OiCq MUPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IH3veZNmKFCDTlOxN|Q{KGOnbHzzJIF1KDNyMDD0c{AyODByIH7NJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYm= M1rwS|I1Ozh6OEC2

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-IκBα / IκBα ; 

PubMed: 25897966     


HeLa cells were pre-treated with RTA 408 or bardoxolone methyl for 6 hours at the indicated concentrations followed by a five-minute treatment with TNFα. Protein levels of phospho-IκBα and total IκBα were evaluated by western blot. Actin was used as loading control. Data are representative of four experiments.

Bcl-xl / Bcl-2 / Bax / Cleaved caspase / Cytochrome C / PARP / Cleaved PARP ; 

PubMed: 25733817     


Representative blots of respective proteins measured to show the effect of CDDO-Me treatment on the expression levels of Bcl-xl, Bcl-2, Bax, PUMA, cytochrome c, cleaved caspase-3 (active), cleaved caspase-9 (active), PARP, and cleaved PARP in Ec109 and KYSE70 cells determined using Western blotting analysis. 

p-PI3K / PI3K / p-AMPK / AMPK / p-p38 MAPK / p38 MAPK / p-AKT / AKT / p-mTOR / mTOR; 

PubMed: 25733817     


Effects of CDDO-Me treatment on the expression levels of p-PI3K at Tyr458, PI3K, p-AMPK at Thr172, AMPK, p-p38 at Thr180, p38, p-Akt at Ser473, Akt, p-mTOR at Ser2448, mTOR, PTEN, beclin 1, LC3-I, and LC3-II in Ec109 and KYSE70 cells. Cellular lysates were analyzed by immunoblotting with respective first antibody followed by the second antibody. 

PTEN / PP2A / PHLPP1 ; 

PubMed: 22177954     


LNCaP and PC-3 cells were treated with CDDO-Me (0.3-5 µM) for 20 h and cell lysates were analyzed for PTEN, PP2A and PHLPP1 by immunoblotting. 

25897966 25733817 22177954
Immunofluorescence
PDI / SDHA ; 

PubMed: 26053096     


MDA-MB 435 cells were treated with or without 1.5 μM CDDO-Me for indicated time points. Immunocytochemistry using anti-PDI (red) and anti-SDHA (green) antibodies was performed and the representative fluorescence and phase contrast microscopic images of cells are shown. Scale bar: 20 μm.

c-PARP / Cytochrome C / COX IV; 

PubMed: 26053096     


E, F. MDA-MB 435 cells were untreated or treated with 1.5 μM CDDO-Me for 24 h. Immunocytochemistry of the cleaved PARP and staining with DAPI were performed (E). Immunocytochemistry of the cytochrome c (Cyt.c) and the subunit I of cytochrome c oxidase (COX IV) was performed (F) Representative fluorescence microscopic images of cells are shown. Scale bars: 50 μm.

26053096
Growth inhibition assay
Cell viability ; 

PubMed: 25733817     


(A) The chemical structure of CDDO-Me and (B) effects of CDDO-Me on the proliferation of Ec109, KYSE70, and Het-1A cells determined by the MTT assay. Notes: Cells were treated with CDDO-Me at 0.01, 0.05, 0.25, 1.0, and 5.0 μM for 24 or 48 hours. Data are the mean ± SD of at least four independent experiments.

25733817
体内研究

Bardoxolone Methyl(60 mg/kg)体内用药,可减少肺肿瘤的数量,大小和降低严重程度。 [4] Bardoxolone Methyl还可显著降低LPS刺激下的体内炎症因子的反应,诱导脾脏HO-1蛋白表达,对抗致死剂量的LPS保护小鼠。 [5]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:

[3]

- 合并

IKK 试验:

对IKK进行分析,以确定CDDO-ME对TNF诱导的IKK活化的效果。简言之,从全细胞提取物的IKK复合物与针对IKKα和IKKβ抗体沉淀,然后用蛋白A / G琼脂糖珠进行处理。 2小时后,用裂解缓冲液清洗珠粒,然后悬浮在含有50 mmol/L HEPES (pH 7.4) 的激酶测定混合物中,20 mmol/L MgCl2,2 mmol / L的DTT,2 mmol/L DTT, 20 μCi [γ-32P]ATP,10 μmol/L未标记的ATP和2 μg谷胱甘肽S-转移酶- IκBα(氨基酸1-54)的底物。在30℃下进行温育30分钟,然后加入SDS缓冲液,沸浴5分钟终止该反应。最后,该蛋白在10%SDS-PAGE凝胶中分离,干燥,用Storm820观察记录放射性条带。为了确定每个样品中的IKK-α和IKK-β的总量,将50 μg的全细胞蛋白在7.5%的SDS-PAGE下解析,电子转移至硝酸纤维素膜上,然后与抗-IKK-α或抗-IKK-β的抗体印迹杂交。
细胞实验:

[2]

- 合并
  • Cell lines: HL-60, KG-1, 和 NB4 细胞
  • Concentrations: ~5 μM
  • Incubation Time: 72 小时
  • Method:

    白血病细胞系以3.0 × 105 cells/mL的密度进行培养,同时白血病单核细胞以5 × 105 cells/mL的密度置于存在或不存在显示浓度的CDDO-ME中培养。加入适量的 DMSO(终浓度小于0.05%)作为对照。添加1 μM ara-C到培养基,用以细胞毒性研究。 24至72小时后,用血细胞计数板的台盼蓝染料排除法进行存活细胞计数。


    (Only for Reference)
动物实验:

[4]

- 合并
  • Animal Models: 雌性 A/J 小鼠 腹腔注射 Vinyl carbamate.
  • Dosages: ~60 mg/kg
  • Administration: 口服给药
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 21 mg/mL (41.52 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
4%DMSO+30% PEG300+5% Tween+61%ddH2O
2.5mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 505.69
化学式

C32H43NO4

CAS号 218600-53-4
储存条件 粉状
溶于溶剂
别名 RTA 402, TP-155, NSC 713200, CDDO Methyl Ester, CDDO-Me

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02316821 Completed Drug: RTA 402|Drug: Placebo Chronic Kidney Disease|Type 2 Diabetes Kyowa Kirin Co. Ltd. December 2014 Phase 2
NCT01598363 Completed Drug: Digoxin|Drug: Rosuvastatin Healthy Volunteers Reata Pharmaceuticals Inc. June 2012 Phase 1
NCT01551446 Withdrawn Drug: Bardoxolone Methyl Renal Insufficiency Chronic|Diabetes Mellitus Type 2 Reata Pharmaceuticals Inc. April 2012 Phase 1
NCT01503866 Completed Drug: bardoxolone methyl Healthy Reata Pharmaceuticals Inc. December 2011 Phase 1
NCT01461161 Completed Drug: bardoxolone methyl Healthy Volunteers Reata Pharmaceuticals Inc. October 2011 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID