142715-48-8
142715-48-8 結(jié)構(gòu)式
基本信息
4-(6,7-二甲氧基-3,4-二氫異喹啉-2(1H)-基)-N-(3,4-二甲氧基苯乙基)-6,7-二甲氧基喹唑啉-2-胺鹽酸鹽
4-(3,4-Dihydro-6,7-diMethoxy-2(1H)-isoquinolinyl)-N-[2-(3,4-diMethoxyphenyl)ethyl]-6,7-diMethoxy-2-quinazolinaMine Monohydrochloride
常見問題列表
IC50: 0.5 μM (MDR1), 1.5 μM (BCRP) in MDCKII cells
CP-100356 (0.1-15 μM； pretreated for 30 min) inhibits acetoxymethyl Calcein (Calcein-AM) uptake and and Digoxin transport in human MDR1-transfected MDCKII cells, with IC
50
s of 0.50 μM and 1.2 μM, respectively. CP-100356 decreases the BCRP-mediated transport of Prazosin in MDCKII cells, with an IC
50
of 1.5 μM.
CP-100356 (0.064-200 μM； 5 min) inhibits OATP1B1-mediated uptake of Estradiol 17β-D-Glucuronide, with an IC
50
of ~66 μM.
CP-100356 (0-50 μM； 10-30 min) is devoid of inhibition (IC
50
>50 μM) against the catalytic activity of the individual P450 enzymes including P4503A4 in the competitive inhibition study.
CP-100356 (6-24 mg/kg; p.o.) increases the systemic exposure of Fexofenadine (36- and 80-fold increase in C max and AUC at the dose of 24 mg/kg) in rats.