1. Membrane Transporter/Ion Channel
  2. P-glycoprotein
  3. Valspodar

Valspodar  (Synonyms: 伐司扑达; PSC 833)

目录号: HY-17384 纯度: ≥98.0%
COA 产品使用指南

Valspodar (PSC 833) 是一种选择性的 P-糖蛋白抑制剂,已被用作化学增敏剂用于实验性癌症的研究。

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Valspodar Chemical Structure

Valspodar Chemical Structure

CAS No. : 121584-18-7

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Top Publications Citing Use of Products

    Valspodar purchased from MCE. Usage Cited in: J Drug Target. 2016;24(5):441-9.  [Abstract]

    Cells are co-treated with 5 μM of free LY156758 or an equivalent dose of SMA-LY156758 and either vehicle control (0.01% DMSO), Elacridar (1 μM), KO143 (5 μM), Valspodar (1 μM) or a combination of efflux inhibitors for 6 h.

    Valspodar purchased from MCE. Usage Cited in: Oncotarget. 2016 Oct 18;7(42):68623-68637.  [Abstract]

    The effect of MDR1 on drug sensitivity to 5-FU in BGC-823 cells is tested by using MDR1 specific inhibitor PSC833. Cells are exposed to 2 μM 5-FU combined with PSC833 (0, 1, 3, 9 μM) for 72 h. Cell viability is detected by CCK-8 assay.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Valspodar (PSC 833) is a selective P-glycoprotein inhibitor that has been used as an experimental cancer treatment and chemosensitizer.

    体外研究
    (In Vitro)

    Valspodar (PSC 833) has no cytotoxicity effects at up to the concentration of 0.75 μg/mL. Valspodar (0.25, 0.5 and 0.75 μg/mL) and DOX-L are added to the DOX resistant cells, and cell kill efficacy of MDR cell type increases significantly when valspodar is administered alongside DOX-L. Valspodar (0.5 and 0.75 μg/mL), in combination with all concentrations of DOX, are most toxic and kill more than 70% of the resistant cells[1].
    Pretreatment with PSC833 decreases the IC50 value of NSC 279836 in MDA-MB-435mdr cells to 0.4±0.02 μM in MDR cells and almost completely reverses the resistance of MDR cells to NSC 279836[3].

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

    体内研究
    (In Vivo)

    valspodar (10 mg/kg, o.p.) exhibits minimal blood-cell partitioning as reflected in its low mean blood-to-plasma ratio of approximately 0.52. Valspodar displays properties of slow clearance and a large volume of distribution. Valspodar shows properties of low hepatic extraction and wide distribution, similar to that of its structural analogue CsA[2].
    Preadministration of PSC833 to mice increases NSC 279836 fluorescent intensity in MDR tumor to 94% of that in the wild-type tumors[3].

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

    Clinical Trial
    分子量

    1214.62

    Formula

    C63H111N11O12

    CAS 号
    性状

    固体

    颜色

    White to yellow

    中文名称

    伐司朴达

    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 6 months
    -20°C 1 month
    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 100 mg/mL (82.33 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 0.8233 mL 4.1165 mL 8.2330 mL
    5 mM 0.1647 mL 0.8233 mL 1.6466 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, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1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    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (2.06 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,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 25.0 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: 99.27%

    参考文献
    Cell Assay
    [1]

    The in vitro cytotoxicity of various formulations against T47D/TAMR-6 cells is investigated by MTT assay. A 104 T47D/TAMR-6 cells are cultured in 96-well plate containing RPMI medium and incubated overnight to allow cell attachment. After 48 hours incubation, fresh medium containing serial concentration of various drug formulations, including free DOX, DOX-L, mixture of DOX-L and free Valspodar (PSC 833), mixture of DOX-L and PSC-L and DOX/PSC-L are added. The plates are then incubated for an additional 48 hours before washing with normal saline followed by adding MTT solution (0.5 mg/mL) to each well, and incubated for 4 h at 37°C. Then, the medium is removed, and DMSO is added to dissolve the formazan crystals. The plates are mildly shaken for 10 min to ensure the dissolution of formazan. The formazan dye is measured spectrophotometrically using microplate reader at 570 nm with reference standard of 690 nm as described before.

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

    Animal Administration
    [2]

    Male Sprague–Dawley rats (250-350 g) are housed in temperature-controlled rooms with 12 h of light per day. The animals had free access to food and water prior to experimentation. Rats are divided into two groups: one group (n=6) receives intravenous dose (5 mg/kg) of valspodar and the other group administered valspodar orally (10 mg/kg). Stereoselective pharmacokinetics of desbutylhalofantrine, a metabolite of halofantrine, in the rat after administration of the racemic metabolite or parent drug. After surgery, the rats are transferred to their regular holding cages and allowed free access to water, but food is withheld overnight. The next morning, rats are transferred to the metabolic cages and dosed with valspodar.

    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, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1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 0.8233 mL 4.1165 mL 8.2330 mL 20.5826 mL
    5 mM 0.1647 mL 0.8233 mL 1.6466 mL 4.1165 mL
    10 mM 0.0823 mL 0.4117 mL 0.8233 mL 2.0583 mL
    15 mM 0.0549 mL 0.2744 mL 0.5489 mL 1.3722 mL
    20 mM 0.0412 mL 0.2058 mL 0.4117 mL 1.0291 mL
    25 mM 0.0329 mL 0.1647 mL 0.3293 mL 0.8233 mL
    30 mM 0.0274 mL 0.1372 mL 0.2744 mL 0.6861 mL
    40 mM 0.0206 mL 0.1029 mL 0.2058 mL 0.5146 mL
    50 mM 0.0165 mL 0.0823 mL 0.1647 mL 0.4117 mL
    60 mM 0.0137 mL 0.0686 mL 0.1372 mL 0.3430 mL
    80 mM 0.0103 mL 0.0515 mL 0.1029 mL 0.2573 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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