产品名称

依克立达盐酸盐(Elacridar HCl)

一般描述

Elacridar HCl (依克立达盐酸盐) is a potent P-gp (MDR-1) and BCRP inhibitor.

别 称

N-[4-[2-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)ethyl]phenyl]-5-methoxy-9-oxo-10H-acridine-4-carboxamide;  hydrochloride; Elacridar hydrochloride.

纯 度

≥98%(HPLC)

CAS NO.

143851-98-3

分子式

C³⁴H³⁴ClN³O⁵

分子量

600.112

适用范围

生物试剂，适用于细胞培养等

l  理化信息

外 观

黄色固体

l  生物学信息

生物活性/药理作用

Elacridar is an oral bioenhancer that targets multiple drug resistance in tumors. In many cases, the appearance of multidrug resistance in cancer is due to a change in of protein inhibitors.

P-glycoprotein is a well characterized human ABC-transporter of the MDR/TAP subfamily. It is an ATP-dependent efflux pump with broad substrate specificity. It likely evolved as a defence  mechanism against harmful substances. Increased intestinal of  P-glycoprotein can reduce the absorption of drugs that are substrates for P-glycoprotein. Thus, there is a reduced bioavailability, therapeutic plasma concentrations are not attained. Elacridar functions by inhibiting P-glycoprotein, resulting in an increased bioavailability of coadminstered drugs.

l  包装与存储

包 装

5mg; 25mg; 100mg

存储温度

0-5℃

l  注意事项及免责声明

本产品仅用于实验研究，不得作为药物使用，不得用于家用或其它用途。

l  参考文献

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.   https://www.ncbi.nlm.nih.gov