1. Immunology/Inflammation Metabolic Enzyme/Protease
  2. AP-1 MMP
  3. T-5224

T-5224 是选择性的转录因子 c-Fos/activator protein (AP)-1 抑制剂,具有抗炎活性,能特异性抑制 c-Fos/c-Jun 的 DNA 结合活性,而不影响其他转录因子的结合活性。T-5224 抑制 IL-1β 诱导的 Mmp-3、Mmp-13、Adamts-5 转录上调。

MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

T-5224 Chemical Structure

T-5224 Chemical Structure

CAS No. : 530141-72-1

1.  客户无需承担相应的运输费用。

2.  同一机构(单位)同一产品试用装仅限申领一次,同一机构(单位)一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1252
In-stock
5 mg ¥1100
In-stock
10 mg ¥1650
In-stock
50 mg ¥3950
In-stock
100 mg ¥5950
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

注册 MCE会员完成审核
即刻享有 积分商城 300 专属积分

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 47 篇科研文献

WB

    T-5224 purchased from MCE. Usage Cited in: Biochem Pharmacol. 2018 Sep;155:275-287.  [Abstract]

    Twist1, nuclear NF-κB-p65 and secreted TNF-α in macrophages after transfection with Twist1 siRNA (100 pmol/well) for 48 h and then treatment with LPS, TT-TFM (200 μM) and T5224 (50 μM) for another 24 h.

    T-5224 purchased from MCE. Usage Cited in: Endocrinology. 2017 Nov 1;158(11):4064-4075.  [Abstract]

    Cyp27b1 induction by LPS or TNF-α is mediated by NF-κB. HCT116 cells are treated with 100 ng/mL LPS or 100 ng/mL TNF-α overnight in the presence or absence of 20 ng/mL T-5224 as indicated. Cyp27b1 protein levels are measured by Western blotting.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    T-5224 is a transcription factor c-Fos/activator protein (AP)-1 inhibitor with anti-inflammatory effects, which specifically inhibits the DNA binding activity of c-Fos/c-Jun without affecting other transcription factors. T-5224 inhibits the IL-1β-induced up-regulation of Mmp-3, Mmp-13 and Adamts-5 transcription[1][2].

    IC50 & Target

    c-Fos/activator protein (AP)-1[1]

    体外研究
    (In Vitro)

    T-5224 inhibits in-vitro production of the mediators MMP-1, MMP-3, IL-6 and TNF-α by IL-1β-stimulated human synovial SW982 cells with the mean IC50 of about 10 μM[2].
    T-5224 (0-80 μM) significantly inhibits the invasion, migration, and MMP activity of HSC-3-M3 cells in a dose-dependent manner[3].

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

    体内研究
    (In Vivo)

    Administration of T-5224 (300 mg/kg, p.o.) after intraperitoneal injection of LPS impartes appreciable protection against acute elevations in serum levels of TNFα, HMGB1, ALT/AST as well as in liver tissue levels of MIP-1α and MCP-1, and reduces the lethality (27%)[4].
    G2 is observed in rat and monkey liver microsomes as a major metabolite of T-5224, suggesting that G2 is not a human-specific metabolite[5].
    T-5224 (300 mg/kg, p.o.) inhibits the production of TNF-alpha and other downstream effectors in C57BL/6 mice[6].

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

    分子量

    517.53

    Formula

    C29H27NO8

    CAS 号
    性状

    固体

    颜色

    White to yellow

    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
    In Vitro: 

    DMSO 中的溶解度 : 100 mg/mL (193.23 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 1.9323 mL 9.6613 mL 19.3225 mL
    5 mM 0.3865 mL 1.9323 mL 3.8645 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)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    In Vivo:

    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    90% (20% SBE-β-CD in Saline)

      Solubility: 5 mg/mL (9.66 mM); 悬浊液; 超声助溶

      此方案可获得 5 mg/mL的均匀悬浊液,悬浊液可用于口服和腹腔注射。

      1 mL 工作液为例,取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

      20% SBE-β-CD in Saline 的配制(4°C,储存一周):2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
    • 方案 二

      请依序添加每种溶剂: 10% DMSO    90% Corn Oil

      Solubility: 5 mg/mL (9.66 mM); 澄清溶液; 超声助溶

      此方案可获得 5 mg/mL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。

      1 mL 工作液为例,取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    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

    g

    每只动物的给药体积

    μL

    动物数量

    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: 99.59%

    参考文献
    Cell Assay
    [4]

    HSC-3-M3 cells are starved for 24 h with DMEM containing 0.5% FBS. The top chamber of the cell invasion device is coated with 50 μL of 0.1 × basement membrane extract solution and incubataed overnight. HSC-3-M3 cells (5.0 × 104 cells/well) are added to the top chamber with DMEM containing 0.5% FBS mixed with 0-80 μM T-5224; DMEM with 10% FBS is added to the bottom chamber and incubated for 48 h. The bottom plate is read using a multilabel plate reader. The data are compared with the standard curve to determine the fraction of invaded cells.

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

    Animal Administration
    [2]

    Mice in LPS group are administered orally with polyvinylpyrrolidone solution in the same volume of T-5224 solution immediately after LPS injection, while in the T-5224 group, mice are administered orally with T-5224 (300 mg/kg, p.o.) in the same manner. In the control group, mice receives polyvinylpyrrolidone solution orally soon after intraperitoneal saline injection. Blood samples are collected for each measurement at the optimal time.

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

    参考文献

    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。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.9323 mL 9.6613 mL 19.3226 mL 48.3064 mL
    5 mM 0.3865 mL 1.9323 mL 3.8645 mL 9.6613 mL
    10 mM 0.1932 mL 0.9661 mL 1.9323 mL 4.8306 mL
    15 mM 0.1288 mL 0.6441 mL 1.2882 mL 3.2204 mL
    20 mM 0.0966 mL 0.4831 mL 0.9661 mL 2.4153 mL
    25 mM 0.0773 mL 0.3865 mL 0.7729 mL 1.9323 mL
    30 mM 0.0644 mL 0.3220 mL 0.6441 mL 1.6102 mL
    40 mM 0.0483 mL 0.2415 mL 0.4831 mL 1.2077 mL
    50 mM 0.0386 mL 0.1932 mL 0.3865 mL 0.9661 mL
    60 mM 0.0322 mL 0.1610 mL 0.3220 mL 0.8051 mL
    80 mM 0.0242 mL 0.1208 mL 0.2415 mL 0.6038 mL
    100 mM 0.0193 mL 0.0966 mL 0.1932 mL 0.4831 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.

    您最近查看的产品:

    Your information is safe with us. * Required Fields.

       产品名称:

     

    * 需求量:

    * 客户姓名:

     

    * Email:

    * 电话:

     

    * 公司或机构名称:

       留言给我们:

    Bulk Inquiry

    Inquiry Information

    产品名称:
    T-5224
    目录号:
    HY-12270
    需求量: