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Merck
CN
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文件

480418

Sigma-Aldrich

NF279

A suramin analog that acts as a highly selective, competitive, and reversible ATP-antagonist of P2X receptor (IC₅₀/KB ~ 1 µM in smooth muscle).

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所有图片(1)
别名:
NF279, 8,8ʹ-(Carbonylbis(imino-4,1-phenylenecarbonylimino-4,1-phenylenecarbonylimino))bis-1,3,5-naphthalenetrisulfonic Acid, Na
经验公式（希尔记法）:
C49H30N6O23S6 · 6Na
CAS号:
202983-32-2
分子量:
1401.12
UNSPSC代码:
12352200
NACRES:
NA.77

质量水平

100

检测方案

≥99% (HPLC)

形式

solid

制造商/商品名称

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°C

InChI

1S/C49H36N6O23S6.6Na/c56-45(50-29-9-1-27(2-10-29)47(58)54-37-17-19-39(81(67,68)69)35-21-33(79(61,62)63)23-41(43(35)37)83(73,74)75)25-5-13-31(14-6-25)52-49(60)53-32-15-7-26(8-16-32)46(57)51-30-11-3-28(4-12-30)48(59)55-38-18-20-40(82(70,71)72)36-22-34(80(64,65)66)24-42(44(36)38)84(76,77)78;;;;;;/h1-24H,(H,50,56)(H,51,57)(H,54,58)(H,55,59)(H2,52,53,60)(H,61,62,63)(H,64,65,66)(H,67,68,69)(H,70,71,72)(H,73,74,75)(H,76,77,78);;;;;;/q;6*+1/p-6

InChI key

RJMCMLNRWDKUDB-UHFFFAOYSA-H

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

包装

Packaged under inert gas

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

WGK

WGK 1

闪点(°F)

Not applicable

闪点(°C)

Not applicable

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