P-gp inhibitor 4

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P-gp inhibitor 4 

P-gp inhibitor 4 (Compound 8b) 是一种选择性的 P-glycoprotein 调节剂，EC50 值为 94 nM。P-gp inhibitor 4 增加药物通过胃肠道屏障的能力，恢复 doxorubicin 在耐药癌细胞中的毒性。

P-gp inhibitor 4

P-gp inhibitor 4 Chemical Structure

CAS No. : 2652001-05-1

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生物活性

P-gp inhibitor 4 (Compound 8b) is a selective P-glycoprotein modulator with an EC50 of 94 nM. P-gp inhibitor 4 increases drug transport across gastro-intestinal barrier and recovers doxorubicin toxicity in multidrug resistant cancer cells[1].

IC50 & Target

EC50: 94 nM (P-glycoprotein)[1]
体外研究
(In Vitro)

P-gp inhibitor 4 (Compound 8b) (0-1 μM, 48 h) significantly increases the cytotoxic effect of antineoplastic drug with co-administration[1].
P-gp inhibitor 4 does not alter the physiological properties of Caco-2 cells barrier model[1].
P-gp inhibitor 4 selectively reduces the activity of P-gp and increases the transport of multiple P-gp substrates across gastro-intestinal barrier[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: MDCK-MDR1
Concentration: 100 nM, 500 nM and 1 μM
Incubation Time: 48 h
Result: Showed no cytotoxicity. Significantly increased the cytotoxic effect of antineoplastic drug.

Cell Viability Assay[1]

Cell Line: Caco-2 cells
Concentration: 0.1 nM-100 µM
Incubation Time: 72 h
Result: Displayed a dose-dependence cytotoxicity that was significant at ≥ 10 μM concentration. Did not reduce cell viability at 100 nM.

分子量

714.85

Formula

C38H38N2O8S2
CAS 号

2652001-05-1
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.
参考文献

  • [1]. Contino M, et al. One molecule two goals: A selective P-glycoprotein modulator increases drug transport across gastro-intestinal barrier and recovers doxorubicin toxicity in multidrug resistant cancer cells. Eur J Med Chem. 2020 Dec 15;208:112843.

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