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CAS No. : 142715-48-8
MCE 国际站:CP-100356 hydrochloride
产品活性:CP-100356 hydrochloride 是一种具有口服活性的 MDR1 (P-gp)/BCRP 双重抑制剂,可以抑制 MDR1 介导的 Calcein-AM 转运 (IC50=0.5 µM) 和 BCRP 介导的 Prazosin 转运 (IC50=1.5 µM)。CP-100356 hydrochloride 也是 OATP1B1 的弱抑制剂 (IC50=∼66 µM)。CP-100356 hydrochloride 对 MRP2 和主要的人 P450 酶没有抑制作用 (IC50>15 µM)。
研究领域:Membrane Transporter/Ion Channel
作用靶点:P-glycoprotein | BCRP
In Vitro: 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 IC50s of 0.50 μM and 1.2 μM, respectively. CP-100356 decreases the BCRP-mediated transport of Prazosin in MDCKII cells, with an IC50 of 1.5 μM.
?CP-100356 (0.064-200 μM; 5 min) inhibits OATP1B1-mediated uptake of Estradiol 17β-D-Glucuronide, with an IC50 of ~66 μM.
?CP-100356 (0-50 μM; 10-30 min) is devoid of inhibition (IC50>50 μM) against the catalytic activity of the individual P450 enzymes including P4503A4 in the competitive inhibition study.
In Vivo: CP-100356 (6-24 mg/kg; p.o.) increases the systemic exposure of Fexofenadine (36- and 80-fold increase in Cmax and AUC at the dose of 24 mg/kg) in rats.
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