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

P-gp inhibitor 1 

目录号: HY-101791 纯度: 98.79%
产品使用指南

P-gp inhibitor 1是一种新型的可逆转P-糖蛋白介导的多药耐药性抑制剂。

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P-gp inhibitor 1 Chemical Structure

P-gp inhibitor 1 Chemical Structure

CAS No. : 2050747-49-2

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生物活性

P-gp inhibitor 1 is a novel inhibitor reversing P-glycoprotein-mediated multidrug resistance.

IC50 & Target

P-glycoprotein[1]

体外研究
(In Vitro)

P-gp inhibitor 1 (12k) possesses high potency (EC50=57.9±3.5 nM), low cytotoxicity, and long duration of activity in reversing doxorubicin (DOX) resistance in K562/A02 cells (1 μM, 80 minutes)[1].

P-gp inhibitor 1 also boosts the potency of other MDR-related cytotoxic agents with different structures, increases accumulation of DOX, blocks Pgp-mediated Rh123 efflux, and suppresses P-gp ATPase activity in K562/A02 MDR cells (0.1, 1, 5 μM, 1 hour)[1].

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

Western Blot Analysis[1]

Cell Line: K562/A02 cell
Concentration: 0.1, 0.5, or 2.0 μM
Incubation Time: 72 hours
Result: MDR reversal by 12k was not caused by a decreased protein expression but instead most likely due to direct inhibition of P-gp efflux[1].
分子量

517.62

Formula

C32H31N5O2

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

DMSO : 16.67 mg/mL (32.21 mM; ultrasonic and warming and heat to 70°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9319 mL 9.6596 mL 19.3192 mL
5 mM 0.3864 mL 1.9319 mL 3.8638 mL
10 mM 0.1932 mL 0.9660 mL 1.9319 mL
*

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 (protect from light)。-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。

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 *
= × ×

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

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P-gp inhibitor 1
目录号:
HY-101791
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