1. Membrane Transporter/Ion Channel
  2. P-glycoprotein
  3. KR30031

KR30031 是一种 Verapamil (HY-14275) 类似物,也是一种具有口服活性的 P-glycoprotein (P-gp) 抑制剂。KR30031 通过抑制 P-gp 增强抗癌剂的细胞毒性,且心血管不良反应较少。KR30031 可用于研究癌症中的多药耐药 (MDR) 逆转。

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KR30031

KR30031 Chemical Structure

CAS No. : 205535-74-6

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

KR30031, a Verapamil (HY-14275) analog, is an orally active P-glycoprotein (P-gp) inhibitor. KR30031 enhances the cytotoxicity of anticancer agents by inhibiting P-gp with fewer cardiovascular adverse effects. KR30031 can be used to study multidrug resistance (MDR) reversal in cancer[1][2].

体外研究
(In Vitro)

KR30031 (0.01-100 μM) 可浓度依赖性地舒张经 60 mM KCl 预收缩的主动脉,其 EC50 为 9.14 μM[1]
KR30031 (0.0001-100 mM) 可浓度依赖性地降低离体心脏的左心室压 (LVP),其 EC50 为 11.6 mM 并且还可浓度依赖性地降低离体心脏的心率 (HR)[1]
KR30031 (0.3-10.0 μM, 72 h) 可增强 Paclitaxel (HY-B0015)对高表达 P-糖蛋白的 HCT15/CL02 细胞和 MES-SA/DX5 细胞的细胞毒性,其 IC50 分别为 3.20 μM 和 7.63 μM[1]
KR30031 (0.3-100 μM, 72 h) 仅在 100 μM 时对 HCT15/CL02 细胞和 MES-SA/DX5 细胞表现出内在细胞毒性[1]
KR30031 (25 μM) 可增加 Paclitaxel 在 Caco-2 细胞单层中的顶侧到基底侧转运,其效力与 Verapamil (HY-14275) 相当[2]

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

体内研究
(In Vivo)

KR30031 (术后 40 分钟开始,每 5 分钟静脉注射一次) 可使麻醉大鼠的平均动脉压 (MAP) 呈剂量依赖性降低,其 ED20 为 0.842 mg/kg,还可呈剂量依赖性减慢心率 (HR),其 ED20 为 2.588 mg/kg[1]

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

分子量

438.56

Formula

C26H34N2O4

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:
KR30031
目录号:
HY-123384
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