产品说明
一般描述
A suramin analog that acts as a highly selective, competitive, and reversible ATP-antagonist of P2X receptor (IC50/KB ~1 µM in smooth muscle). Effectively discriminates between P2Y and P2X receptors with no discernible effects on α1A adrenoceptors, adenosine A1 and A2B receptors, histamine H1, muscarinic M3 and neuronal nicotinic acetylcholine receptors. Displays a selectivity profile of P2X1 >P2X2 >P2X3 >P2X4 (IC50 = 19 nM, 770 nM, 1.62 µM and >300 µM, respectively) in Xenopus oocytes 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 µM in smooth muscle). Effectively discriminates between P2Y and P2X receptors with no effect on α1A adrenoceptors, adenosine A1 and A2B receptors, histamine H1, muscarinic M3 and neuronal nicotinic acetylcholine receptors. Displays a selectivity profile of P2X1 >P2X2 >P2X3 >P2X4 (IC50 = 19 nM, 770 nM, 1.62 µM and >300 µM, respectively) in Xenopus oocytes 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 µM as antagonist of P2X receptor in smooth muscle; 19 nM, 770 nM, 1.62 µM and <300 µM, 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 |
产品性质
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 |