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

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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10 mM * 1 mL in DMSO ¥1025
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1 mg ¥398
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5 mg ¥900
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10 mg ¥1440
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25 mg ¥2710
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50 mg ¥3920
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100 mg ¥5536
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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

IC50 & Target

P-glycoprotein[1]

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HUVEC IC50
73.58 μM
Compound: 12k
Cytotoxicity against HUVEC assessed as reduction in cell viability after 48 hrs by MTT assay
Cytotoxicity against HUVEC assessed as reduction in cell viability after 48 hrs by MTT assay
[PMID: 28355069]
K562 IC50
4 μM
Compound: 12k
Cytotoxicity against human K562 cells assessed as suppression of cell viability after 48 hrs by MTT assay
Cytotoxicity against human K562 cells assessed as suppression of cell viability after 48 hrs by MTT assay
[PMID: 28355069]
K562/A02 IC50
12.78 μM
Compound: 12k
Cytotoxicity against human K562/A02 cells assessed as suppression of cell viability after 48 hrs by MTT assay
Cytotoxicity against human K562/A02 cells assessed as suppression of cell viability after 48 hrs by MTT assay
[PMID: 28355069]
体外研究
(In Vitro)

P-gp抑制剂1 (12k) 在逆转K562/A02细胞中的多柔比星(DOX)耐药性方面表现出高效力(EC50=57.9±3.5 nM)、低细胞毒性和长时间的活性(1 μM,80分钟)[1]
此外,P-gp抑制剂1还能增强其他结构不同的多药耐药(MDR)相关细胞毒性药物的效果,增加DOX的累积量,阻止P-糖蛋白介导的Rh123外排,并抑制P-糖蛋白的ATP酶活性(在K562/A02 MDR细胞中,浓度为0.1, 1, 5 μM,作用时间为1小时)[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
性状

固体

颜色

Light yellow to brown

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
细胞实验: 

DMSO 中的溶解度 : 16.67 mg/mL (32.21 mM; 超声助溶 (<70°C); 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 1.9319 mL 9.6596 mL 19.3192 mL
5 mM 0.3864 mL 1.9319 mL 3.8638 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 (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。

  • 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

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
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 (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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9319 mL 9.6596 mL 19.3192 mL 48.2980 mL
5 mM 0.3864 mL 1.9319 mL 3.8638 mL 9.6596 mL
10 mM 0.1932 mL 0.9660 mL 1.9319 mL 4.8298 mL
15 mM 0.1288 mL 0.6440 mL 1.2879 mL 3.2199 mL
20 mM 0.0966 mL 0.4830 mL 0.9660 mL 2.4149 mL
25 mM 0.0773 mL 0.3864 mL 0.7728 mL 1.9319 mL
30 mM 0.0644 mL 0.3220 mL 0.6440 mL 1.6099 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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P-gp inhibitor 1
目录号:
HY-101791
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