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

Zosuquidar trihydrochloride  (Synonyms: 唑喹达三盐酸盐; RS 33295-198 trihydrochloride; LY-335979 trihydrochloride)

目录号: HY-50671 纯度: 99.79%
COA 产品使用指南

Zosuquidar (LY335979) trihydrochloride 是一种 P-糖蛋白 (P-gp) 抑制剂 (Ki=59 nM)。Zosuquidar trihydrochloride 具有抗肿瘤活性,并可用于急性骨髓性白血病 (AML) 的研究。

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Zosuquidar trihydrochloride Chemical Structure

Zosuquidar trihydrochloride Chemical Structure

CAS No. : 167465-36-3

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Other Forms of Zosuquidar trihydrochloride:

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Top Publications Citing Use of Products

    Zosuquidar trihydrochloride purchased from MCE. Usage Cited in: J Pharm Biomed Anal. 2012 Jul;66:232-9.  [Abstract]

    Effect of pharmacological inhibition of drug efflux transporters on brain distribution of FLZ in rats. The rats receive 35 mg/kg FLZ via tail vein injection 10 min after intravenous administration of 20 mg/kg Zosuquidar or 7.5 mg/kg ko143.
    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Zosuquidar (LY335979) trihydrochloride is a P-glycoprotein (P-gp) inhibitor (Ki=59 nM). Zosuquidar trihydrochloride shows anti-tumor activities, and can be used in acute myelogenous leukemia (AML) research[1][2][3].

    IC50 & Target

    Ki: 59nM (P-glycoprotein)[1].

    体外研究
    (In Vitro)

    Zosuquidar (0.3 μM; 48 h) enhances the cytotoxicity of DNR (substrates for P-glycoproteins) in P-glycoproteins active cell lines[2].
    ? Zosuquidar (5-16 μM; 72 h) treatment alone shows high cytotoxic concentration to drug-sensitive and MDR cell lines[1].

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

    Cell Cytotoxicity Assay[2]

    Cell Line: K562 and HL60 cells
    Concentration: 0.3 μM
    Incubation Time: 48 hours
    Result: Enhanced the cytotoxicity of DNR (substrates for P-glycoproteins) in K562/DOX cells more than 45.5-fold.

    Cell Cytotoxicity Assay[1]

    Cell Line: CCRF-CEM, CEM/VLB100, P388, P388/ADR, MCF7, MCF7/ADR, 2780, 2780AD, UCLA-P3, UCLA-P3.003VLB cells
    Concentration: 5-16 μM
    Incubation Time: 72 hours
    Result: Showed IC50s of 6, 7, 15, 8, 7, 15, 11, 16, >5, >5 μM for CCRF-CEM, CEM/VLB100, P388, P388/ADR, MCF7, MCF7/ADR, 2780, 2780AD, UCLA-P3, UCLA-P3.003VLB cells, respectively.
    体内研究
    (In Vivo)

    Zosuquidar (intraperitoneal injection; 30, 10, 3, or 1 mg/kg; once daily; 5 d) treatment shows a significant increase in life span[1].
    ? Zosuquidar (intraperitoneal injection; 30 mg/kg; once daily; 5 d) treatment shows the potentiation with a combined of Doxorubicin[1].

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

    Animal Model: Mice implanted with P388/ADR tumors[1]
    Dosage: 30, 10, 3, or 1 mg/kg
    Administration: Intraperitoneal injection; 30, 10, 3, or 1 mg/kg; once daily; 5 days
    Result: Exihibited a significantly increased survival compared to the group treated with Doxorubicin alone (P<0.001).
    Animal Model: Mice implanted with P388 or P388/ADR murine leukemia cells[1]
    Dosage: 30 mg/kg
    Administration: Intraperitoneal injection; 30 mg/kg; once daily; 5 days
    Result: Observed significant antitumor activity against the MDR P388/ADR cell lines when mice were treated with a combined dose of 30 mg/kg LY335979 and 1 mg/kg Doxorubicin (P=0.1).
    Clinical Trial
    分子量

    636.99

    Formula

    C32H34Cl3F2N3O2

    CAS 号
    性状

    固体

    颜色

    Light yellow to yellow

    中文名称

    唑喹达三盐酸盐

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    4°C, sealed storage, away from moisture

    *该产品在溶液状态不稳定,建议您现用现配,即刻使用。

    溶解性数据
    In Vitro: 

    H2O 中的溶解度 : 5 mg/mL (7.85 mM; 超声助溶)

    DMSO 中的溶解度 : 1 mg/mL (1.57 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 1.5699 mL 7.8494 mL 15.6988 mL
    5 mM 0.3140 mL 1.5699 mL 3.1398 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;该产品在溶液状态不稳定,建议您现用现配,即刻使用。

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

    • 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:

    以下溶解方案源自文献,仅供参考,建议您先取少量样品进行尝试。

    • 方案 一

      Zosuquidar is dissolved in 20% ethanol-saline[5].

    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
    计算结果
    工作液所需浓度 : mg/mL
    纯度 & 产品资料

    纯度: 99.79%

    参考文献

    Zosuquidar trihydrochloride 相关分类

    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;该产品在溶液状态不稳定,建议您现用现配,即刻使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO / H2O 1 mM 1.5699 mL 7.8494 mL 15.6988 mL 39.2471 mL
    H2O 5 mM 0.3140 mL 1.5699 mL 3.1398 mL 7.8494 mL

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

    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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    产品名称:
    Zosuquidar trihydrochloride
    目录号:
    HY-50671
    需求量: