半岛bd体育手机客户端 说明
生化/生理作用
Draflazine (R88021; (-)-R75231), is a potent nucleoside transporter ENT1 (SLC29A1) inhibitor with 370-fold selectivity over ENT2 (SLC29A2). R88021 exhibits 30- and 40-times higher affinity as (+)-R75231 (R88016) using calf lung membrane preparation (by [3H]R75231 & [3H]NBI displacement) and intact human erythrocytes (by [3H]NBMPR displacement), respectively. Draflazine is 20-times more potent as R88016 in enhancing adenosine potency against ADP-induced aggregation in human whole blood (IC50 = 0.5 μM vs 10 μM with 1 μM respective inhibitor), Draflazine and R75231, but not R88016, show cardioprotective efficacy against catecholamines infusion in rabbitsin vivo.
基本信息
经验(实验)分子式 | C30H33Cl2F2N5O2 |
分子量 | 604.52 |
半岛bd体育手机客户端 性质
测定 | ≥98% (HPLC) |
形式 | powder |
旋光性 | [α]/D -23 to -29°, c = 0.5 in ethanol |
颜色 | white to beige |
溶解性 | DMSO: 2 mg/mL, clear |
储存温度 | room temp |
InChI | 1S/C30H33Cl2F2N5O2/c31-25-15-23(35)16-26(32)29(25)37-28(40)18-39-14-13-38(17-27(39)30(36)41)12-2-1-3-24(19-4-8-21(33)9-5-19)20-6-10-22(34)11-7-20/h4-11,15-16,24,27H,1-3,12-14,17-18,35H2,(H2,36,41)(H,37,40) |
InChI key | IWMYIWLIESDFRZ-UHFFFAOYSA-N |
安全信息
储存分类代码 | 11 - Combustible Solids |
WGK | WGK 3 |
闪点(F) | Not applicable |
闪点(C) | Not applicable |
Sigma-Aldrich