| 货号 | 4193/50 |
| 别名 | 4-(3,4-Dihydro-6,7-dimethoxy-2(1H)- |
| 供应商 | Tocris |
| 生物活性 | High affinity P-glycoprotein (P-gp) inhibitor (Ki values are 58 and 94 nM for mouse Pgp1a and Pgp1b isoforms). Inhibits calcein-AM uptake in MDR1-transfected MDCKII cells (IC50 = 0.5 μM) and prazosin transport in BCRP-transfected MDCKII cells (IC50 = 1.5 μM). Displays weak or no inhibitory activity against MRP1, OATP1B1 and several major human P450 enzymes (IC50 > 50 μM). |
| 运输条件 | Blue Ice |
| 存放说明 | Ambient |
| 纯度 | >98 % |
| 计算分子量 | 597.1 |
| 分子式 | C31H36N4O6 |
| 可溶性/溶解性 | Soluble to 20 mM in DMSO |
| 参考文献 | Kalgutkaret al(2009)N-(3,4-dimethoxyphenethyl)-4-(6,7-dimethoxy-3,4-dihydroisoquinolin-2[1H]-yl)-6,7-dimethoxyquinazolin-2-amine (CP-100,356) as a "chemical knock-out equivalent" to assess the impact of efflux transporters on oral drug absorption in the rat. J.Pharm.Sci. 98 4914. PMID: 19373887. Tayloret al (1999) The equilibrium and kinetic drug binding properties of the mouse P-gp1a and P-gp1b P-glycoproteins are similar. Br.J.Cancer 81 783. PMID: 10555746. Wandelet al (1999) P-glycoprotein and cytochrome P-450 3A inhibition: dissociation of inhibitory potencies. Cancer Res. 59 3944. PMID: 10463589. |