半岛bd体育手机客户端 说明
一般描述
A suramin analog that acts as a highly selective, competitive, and reversible ATP-antagonist of P2X receptor (IC50/KB~1 ?M in smooth muscle). Effectively discriminates between P2Y and P2X receptors with no discernible effects on α1Aadrenoceptors, adenosine A1and A2Breceptors, histamine H1, muscarinic M3and neuronal nicotinic acetylcholine receptors. Displays a selectivity profile of P2X1>P2X2>P2X3>P2X4(IC50= 19 nM, 770 nM, 1.62 ?M and >300 ?M, respectively) inXenopusoocytes pre-incubated with ATP. In rat and human tissues, exhibits a potency profile of rat P2X1> human P2X1? rat P2X2> rat P2X3~human P2X7? human P2X4. Not degraded by ecto-nucleotidases.
A suramin analog that acts as a highly selective, competitive, and reversible ATP-antagonist of P2X receptor (IC50/KB~ 1 ?M in smooth muscle). Effectively discriminates between P2Y and P2X receptors with no effect on α1Aadrenoceptors, adenosine A1and A2Breceptors, histamine H1, muscarinic M3and neuronal nicotinic acetylcholine receptors. Displays a selectivity profile of P2X1>P2X2>P2X3>P2X4(IC50= 19 nM, 770 nM, 1.62 ?M and >300 ?M, respectively) inXenopusoocytes pre-incubated with ATP. In rat and human tissues, exhibits a potency profile of rat P2X1> human P2X1> > rat P2X2> rat P2X3~ human P2X7> > human P2X4. Not degraded by ecto-nucleotidases.
包装
5 mg in Plastic ampoule
Packaged under inert gas
生化/生理作用
Cell permeable: yes
Product competes with ATP.
Primary Target
P2X receptor
Reversible: yes
Target IC50: ~ 1 ?M as antagonist of P2X receptor in smooth muscle; 19 nM, 770 nM, 1.62 ?M and <300 ?M, against P2X1, P2X2, P2X3, P2X4, respectively, in Xenopus oocytes pre-incubated with ATP
警告
Toxicity: Standard Handling (A)
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.
其他说明
Klapperstück, M., et al. 2000.Eur. J. Pharmacol.387,245.
Rettinger, J., et al. 2000.Neuropharmacol.39,2044.
Lambrecht, G., et al. 1999.Prog. Brain Res.120,107.
Damer, S., et al. 1998.Eur. J. Pharmacol.350,R5.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
基本信息
经验(实验)分子式 | C49H30N6O23S6· 6Na |
分子量 | 1401.12 |
半岛bd体育手机客户端 性质
质量水平 | 100 |
测定 | ≥99% (HPLC) |
形式 | solid |
manufacturer/tradename | Calbiochem? |
储存条件 | OK to freeze desiccated protect from light |
颜色 | white |
溶解性 | DMSO: 14 mg/mL water: 35 mg/mL |
运输 | ambient |
储存温度 | 2-8℃ |
安全信息
储存分类代码 | 11 - Combustible Solids |
WGK | WGK 1 |
闪点(F) | Not applicable |
闪点(C) | Not applicable |
Sigma-Aldrich