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Draflazine
产品别名
138681-29-5
Draflazine
(-)-R 75,231
(-)-R75231
(S)-R-75231
(-)-R 75231
(S)-R 75,231
R 88,021
(-)-R-75231
(S)-2-(Aminocarbonyl)-N-(4-amino-2,6-dichlorophenyl)-4-[5,5-bis(4-fluorophenyl)pentyl]-1-piperazineacetamide
R 88021
(S)-R75231
(S)-R 75231
(-)-1-[2-(4-Amino-2,6-dichloro-anilino)-2-oxo-ethyl]-4-[5,5-bis(4-fluorophenyl)pentyl]piperazine-2-carboxamide
R-88021
R88021
结构式
基本信息
| Empirical Formula【经验(实验)分子式】 | C30H33Cl2F2N5O2 |
| Molecular weight | 604.52 |
| Biochem/physiol Actions【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 rabbits in vivo. |
产品性质
| Assay【测定】 | ≥98% (HPLC) |
| form【形式】 | powder |
| optical activity【旋光性】 | [α]/D -23 to -29°, c = 0.5 in ethanol |
| color【颜色】 | white to beige |
| solubility【溶解性】 | DMSO: 2 mg/mL, clear |
| storage temp.【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
| Storage Class Code【储存分类代码】 | 11 - Combustible Solids |
| WGK | WGK 3 |
