Draflazine

产品名称：

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

产品介绍：

产品说明

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 rabbits in vivo.

基本信息

经验(实验)分子式	C₃₀H₃₃Cl₂F₂N₅O₂
分子量	604.52

产品性质

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