GKT137831

目录号:S7171

GKT137831 Chemical Structure

Molecular Weight(MW): 394.85

GKT137831是一种有效的双NADPH oxidase NOX1/NOX4抑制剂,Ki分别为110 nM和140 nM。对NOX1、4、5的选择性约为对NOX2的10倍,不抑制XO或ROS/RNS。

规格 价格 库存 购买数量  
RMB 1226.73 现货
RMB 3866.86 现货
RMB 8171.12 现货
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客户使用该产品的4个实验数据:

  • Serum markers of liver injury and liver pathology in mice fed control (Ctrl) or ethanol (EtOH) for four weeks with or without GKT137831 for the last two weeks. (A) Light microscopy with hematoxylin & eosin staining shows accumulation of lipid droplets (arrows) and necrosis (arrowheads) in the liver of ethanol-fed mice, which was attenuated by GKT137831 treatment. (B) Serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) activities. Serum ALT and AST activities were measured by using Infinity ALT and AST Reagents. Scale bar: 20μM. Results are mean ± SD (n=6). Results for bars that do not share a letter differed significantly among groups (P <0.05). Significant differences among groups are determined by ANOVA followed by Tukey’s test.

    Biochim Biophys Acta, 2016, 1861(1 Pt A):2912-2921. . GKT137831 purchased from Selleck.

    (C) Indicated macrophages were treated with LPS (100 ng/mL) in the absence or presence of GKT137831 (1 μmol/L) for 24 h. PKM2 mRNA and lactate levels were assayed (n = 3, *, p < 0.05 versus LPS group).

    Mol Med, 2016, doi: 10.2119/molmed.2015.00250. GKT137831 purchased from Selleck.

  • A549 cells were treated with GKT137831 (20 µM) or NAC (25 µM) after transfection with NOX4 plasmid for 48 h. Nrf2 expression was analyzed by western blotting (B). NOX4-overexpressed A549 cells were pretreated with MG132 (25 µM) after the addition of NAC or GKT137831 (C).

    Exp Cell Res, 2017, 352(2):245-254. GKT137831 purchased from Selleck.

    AGE3-BSA-induced apoptosis in A7r5 cells was mediated by NAD(P)H oxidase. (a) Cultured A7r5 cells were incubated in calcification medium containing cBSA, or AGE3-BSA (100 µg/mL) in the presence or absence of NAD(P)H oxidase inhibitors including GKT137831 (20 µM) or VAS2870 (10 µM) for three days. Apoptosis was evaluated by TUNEL assay, as described in the Method section. Cells in the culture were identified by nuclear staining with Hoechst, and evaluated under a fluorescence microscope; (b) For quantification, Hoechst and TUNEL double positive cells were counted in 10 random microscopic fields at 200× magnification, and expressed as percent TUNEL positive cells in a culture. Statistical significance of the results was analyzed by one-way ANOVA followed by LDS post-hoc test. Statistical significance was denoted as follows, ** p < 0.001 vs. AGE3-BSA.

    Int J Mol Sci, 2016, 17(9). pii: E1567. GKT137831 purchased from Selleck.

产品安全说明书

NADPH-oxidase抑制剂选择性比较

生物活性

产品描述 GKT137831是一种有效的双NADPH oxidase NOX1/NOX4抑制剂,Ki分别为110 nM和140 nM。对NOX1、4、5的选择性约为对NOX2的10倍,不抑制XO或ROS/RNS。
靶点
NOX1 [1]
(Cell-based assay)
NOX4 [1]
(Cell-based assay)
110 nM(Ki) 140 nM(Ki)
体外研究

在HPAECs 和 HPASMCs中,GKT137831减弱缺氧诱导的H(2)O(2)释放,细胞增殖,和TGF-β1表达,并改善PPARγ表达减少。[2]在人大动脉内皮细胞中,GKT137831也会防止高血糖症应答产生的氧化应激。[3]

体内研究 在WT和SOD1mut小鼠体内,GKT137831 (60 mg/kg i.g.)阻断肝纤维化,并下调氧化应激,炎症和纤维化的发生。[1]在长期低氧环境下的小鼠模型中,GKT137831 (60 mg/kg/d p.o.)也会减弱长期缺氧诱导的右心室肥大,血管重构,肺细胞增生,以及低氧环境下肺PPARγ 和TGF-β表达的改变。 [2]在糖尿病载脂蛋白E不足的小鼠体内,GKT137831 (60 mg/kg/d p.o.)减弱糖尿病加速的动脉粥样硬化。[3]此外,在注入angII的 c-hNox4Tg小鼠体内,GKT137831废止氧化应激的增加,抑制Akt-mTOR 和 NF-κB信号通路,并减弱心脏重塑。[4]

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)

细胞实验:

[2]

+ 展开
  • Cell lines: 低氧 HPASMC 和 HPAECs
  • Concentrations: 20 μM
  • Incubation Time: 72小时
  • Method:

    低氧HPASMC 和 HPAEC增殖使用MTT法测定,通过Western印迹检测增殖细胞核抗原(PCNA)表达,或台盼蓝着色后进行人工细胞计数。Amplex Red过氧化氢/过氧化物酶检测试剂盒用于测量从HPAECs 或 HPASMCs释放到培养基的H2O2。暴露于对照组或低氧环境下72小时后,加入Amplex Red试剂,荧光检测前,细胞恢复到对照组或低氧环境再培养1小时。


    (Only for Reference)
动物实验:

[1]

+ 展开
  • Animal Models: 肝纤维化小鼠模型
  • Formulation: 玉米油
  • Dosages: 每天 60 mg/kg
  • Administration: i.g.
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 78 mg/mL warmed (197.54 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):
2% DMSO+2% Tween 80+30% PEG 300+ddH2O
9mg/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 394.85
化学式

C21H19ClN4O2

CAS号 1218942-37-0
稳定性 powder
in solvent
别名 N/A

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 (g) = 浓度 (mol/L) x 体积 (L) 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 Conditions Sponsor/Collaborators Start Date Phases
NCT03226067 Recruiting Primary Biliary Cirrhosis Genkyotex SA June 26 2017 Phase 2
NCT02010242 Completed Type 2 Diabetes Mellitus With Diabetic Nephropathy Genkyotex Innovation SAS October 2013 Phase 2

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操作手册

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID