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  3. Troglitazone

Troglitazone  (Synonyms: 曲格列酮; CS-045)

目录号: HY-50935 纯度: 98.60%
COA 产品使用指南

Troglitazone 是口服有效的 PPARγ 激动剂,对人和鼠 PPARγ的 EC50 值分别为 550 nM 和 780 nM。Troglitazone 具有抗癌活性,并能预防和抑制 2 型糖尿病发展。

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Troglitazone Chemical Structure

Troglitazone Chemical Structure

CAS No. : 97322-87-7

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥869
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5 mg ¥493
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10 mg ¥790
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50 mg ¥2788
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100 mg ¥4913
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500 mg   询价  

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Top Publications Citing Use of Products

    Troglitazone purchased from MCE. Usage Cited in: Yonsei Med J. 2018 Nov;59(9):1096-1106.   [Abstract]

    MCN and N2a cells are treated with Control (DMSO), Troglitazone (Tro; 20 µM), or GW9662 (10 µM) for 24 h, followed by detection of PPAR-γ protein level via Western blot assay.

    Troglitazone purchased from MCE. Usage Cited in: Breast Cancer Res Treat. 2017 Oct;165(3):517-527.  [Abstract]

    MDA-MB-231 and Hs578T TNBC ‘‘claudin-1-low’’ cells, and the non-tumorigenic human breast epithelial cell line MCF-10A are treated with 20 μM of TGZ, RGZ, D2-TGZ, or DMSO (Ctrl) for 24 h and subjected to western blot analysis with claudin-1 (CLDN1) antibody. α-tubulin is used as loading control.

    查看 PPAR 亚型特异性产品:

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Troglitazone is an orally active PPARγ agonist, with EC50s of 550 nM and 780 nM for human and murine PPARγ receptor, respectively. Troglitazone has anticancer activity, prevents and inhibits the development of type 2 diabetes.

    IC50 & Target[1]

    PPARγ

    550 nM (EC50, Human PPARγ)

    体外研究
    (In Vitro)

    Troglitazone (2-200 μM, 24 h) is cytotoxic to the pancreatic cancer cell lines (MIA Paca2 and PANC-1 cells), with IC50s of 49.9±1.2 and 51.3±5.3 μM, respectively[2].
    Troglitazone (50 μM, 24 h) increases chromatin condensation in MIA Paca2 and PANC-1 cells, enhances the activity of caspase-3 and decreases Bcl-2 expression[2].
    Troglitazone (0-4 μM, 12 h) sensitizes TRAIL-mediated apoptosis in human lung adenocarcinoma cells (A549, HCC-15 and Calu-3)[3].
    Troglitazone (0-4 μM, 12 h) induces autophagy and sensitized apoptosis mediated by TRAIL in A549 cells[1].

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

    体内研究
    (In Vivo)

    Troglitazone (200 mg/kg, p.o., every day for 5 weeks) shows inhibitory effects on the growth of tumor in the MIA Paca2 xenograft model[2].

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

    Clinical Trial
    分子量

    441.54

    Formula

    C24H27NO5S

    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    曲格列酮;特洛格列酮

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    In solvent -80°C 1 year
    -20°C 6 months
    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 125 mg/mL (283.10 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 2.2648 mL 11.3240 mL 22.6480 mL
    5 mM 0.4530 mL 2.2648 mL 4.5296 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, 1 years; -20°C, 6 months。-80°C储存时,请在1年内使用, -20°C储存时,请在6个月内使用。

    • 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    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (5.66 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

      生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.08 mg/mL (4.71 mM); 澄清溶液

      此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 20.8 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。

    以下溶解方案,请直接配置工作液。建议现用现配,在短期内尽快用完。 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: 0.5% CMC-Na  0.5% Tween-80

      Solubility: 10 mg/mL (22.65 mM); 悬浊液; 超声助溶

    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: 98.60%

    参考文献
    Cell Assay
    [2]

    Briefly, cells are seeded into 96-well plates at a density of 1 × 105 cells/well and incubated for 24 h. The cells are treated with Troglitazone in the presence or absence of other chemicals for a further 24 h using FBS-free medium. The assay utilizes the conversion of alamar blue reagent to fluorescent resorufin by metabolically active cells. The resorufin signal is measured at an excitation wavelength of 530 nm and an emission wavelength of 580 nm. The 50% growth inhibitory concentrations (IC50) are calculated according to the sigmoid inhibitory effect model E = IC50 γ/(IC50 γ + Cγ), where E represents the surviving fraction (% of control), C represents the drug concentration in the medium, and γ represents the Hill coefficient. For co-exposure studies, the Troglitazone dosage is set to approximately the IC50 value for each cell line[2].

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

    Animal Administration
    [2]

    Balb/c male mice (4 weeks old) are subcutaneously inoculated in the back with MIA Paca2 cells (5 × 106 cells/100 μL in PBS) 14 days prior to starting Troglitazone administration. Mice are then orally administered 200 mg/kg Troglitazone in 0.5% methylcellulose solution or vehicle daily for 5 weeks. Tumor size is measured bi-dimensionally and the volume is calculated using the formula (length × width2) × 0.5. Body weights of mice are also monitored throughout the experiment[2].

    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, 1 years; -20°C, 6 months。-80°C储存时,请在1年内使用, -20°C储存时,请在6个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.2648 mL 11.3240 mL 22.6480 mL 56.6200 mL
    5 mM 0.4530 mL 2.2648 mL 4.5296 mL 11.3240 mL
    10 mM 0.2265 mL 1.1324 mL 2.2648 mL 5.6620 mL
    15 mM 0.1510 mL 0.7549 mL 1.5099 mL 3.7747 mL
    20 mM 0.1132 mL 0.5662 mL 1.1324 mL 2.8310 mL
    25 mM 0.0906 mL 0.4530 mL 0.9059 mL 2.2648 mL
    30 mM 0.0755 mL 0.3775 mL 0.7549 mL 1.8873 mL
    40 mM 0.0566 mL 0.2831 mL 0.5662 mL 1.4155 mL
    50 mM 0.0453 mL 0.2265 mL 0.4530 mL 1.1324 mL
    60 mM 0.0377 mL 0.1887 mL 0.3775 mL 0.9437 mL
    80 mM 0.0283 mL 0.1416 mL 0.2831 mL 0.7078 mL
    100 mM 0.0226 mL 0.1132 mL 0.2265 mL 0.5662 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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    目录号:
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