NF279 - CAS 202983-32-2 - Calbiochem

别名

NF279 - CAS 202983-32-2 - Calbiochem,8,8ʹ-(Carbonylbis(imino-4,1-phenylenecarbonylimino-4,1-phenylenecarbonylimino))bis-1,3,5-naphthalenetrisulfonic Acid, Na

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 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. 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.

生化/生理作用

Cell permeable: yes Primary Target
P2X receptor Product competes with ATP. 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

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.