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Encequidar mesylate(HM30181(mesylate))
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Encequidar mesylate(HM30181(mesylate))图片
CAS NO:849675-87-2
规格:98%
分子量:784.83
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
Encequidar(mesylate)(HM30181(mesylate))是P-糖蛋白(P-glycoprotein)的有效竞争性抑制剂。
CAS:849675-87-2
分子式:C39H40N6O10S
分子量:784.83
纯度:98%
存储:Store at -20°C

Background:

Encequidar (mesylate) (HM30181 (mesylate)) is a competitive and potent P-glycoprotein inhibitor.


Compared with control (0 nM Encequidar (HM30181)), paclitaxel potently inhibits the survival of K1735 cells by about 65% at 100 nM and 72% at 1000 nM in a dose-dependent manner. Encequidar (HM30181) does not make any significant changes in the survival of K1735 cells. In contrast, bEnd.3 cells do not show any decreases in survival by the paclitaxel treatment without Encequidar (HM30181). However, treatment of 0.1 or 1 nM Encequidar (HM30181) lead to 20 and 42% inhibition of survival at the 100 nM and 1000 nM paclitaxel treatment, respectively[2].


The plasma concentrations of Encequidar (HM30181) are higher for the simultaneous administration with the microcapsule than with the powder; providing significant differences from 1 to 2 h. The microcapsule has about a 1.7-fold faster Tmax and a 1.6-fold higher AUC value compared with the powder (2.5±0.6 vs. 4.3±0.9 h; 107.7±20.1 vs. 64.3±18.0 h ng/mL). The faster and overall improved absorption of Encequidar (HM30181) in microcapsule form might be due to the remarkable enhancement of the aqueous solubility and dissolution resulting from its crystalline conversion to the amorphous form and particle size reduction[1].


[1]. Kim JC, et al. Effect of HM30181 mesylate salt-loaded microcapsules on the oral absorption of paclitaxel as a novel P-glycoprotein inhibitor. Int J Pharm. 2016 Jun 15;506(1-2):93-101. [2]. Joo KM, et al. Response of brain specific microenvironment to P-glycoprotein inhibitor: an important factor determining therapeutic effect of P-glycoprotein inhibitor on brain metastatic tumors. Int J Oncol. 2008 Oct;33(4):705-12.