4-(3,4-Dihydro-6,7-diMethoxy-2(1H)-isoquinolinyl)-N-[2-(3,4-diMethoxyphenyl)ethyl]-6,7-diMethoxy-2-quinazolinaMine Monohydrochloride

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.}