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Merck
CN
所有图片(1)

主要文件

5.08317

Sigma-Aldrich

A740003

别名:

A740003, N-(1-{[(cyanoimino)(5-quinolinylamino) methyl] amino}-2,2-dimethylpropyl)-2-(3,4-dimethoxyphenyl)acetamide, A 740003, P2X7 Purinegic Receptor, A740003, A740003

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About This Item

经验公式(希尔记法):
C26H30N6O3
分子量:
474.55
MDL编号:
UNSPSC代码:
12352200

方案

≥98% (HPLC)

质量水平

表单

powder

效能

18 nM IC50

制造商/商品名称

Calbiochem®

储存条件

OK to freeze
protect from light

颜色

off-white

溶解性

DMSO: 30 mg/mL

储存温度

2-8°C

InChI

1S/C26H30N6O3/c1-26(2,3)24(31-23(33)15-17-11-12-21(34-4)22(14-17)35-5)32-25(29-16-27)30-20-10-6-9-19-18(20)8-7-13-28-19/h6-14,24H,15H2,1-5H3,(H,31,33)(H2,29,30,32)

InChI key

PUHSRMSFDASMAE-UHFFFAOYSA-N

一般描述

A highly potent, selective, competitive antagonist of P2X7 purinegic receptor (IC50 = 18 nM and 40 nM, respectively as measured by Bz-ATP-stimulated Ca2+ flux). Does not affect other P2 receptors even at 10 µM concentrations. Blocks agonist-evoked IL-1b release (IC50 = 156 nM) and pore formation (IC50 = 92 nM) in differentiated human THP-1 cells. Also shown to reduce carrageenan and Freund′s adjuvant -induced thermal hyperalgesia (ED50 = 38-54 mg/kg, i.p) and neuropathic pain induced by chronic constriction injury (CIC) of the sciatic nerve.

生化/生理作用

Primary Target
P2X7

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

制备说明

Slight warming is required for complete solubilization.

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

其他说明

Honore, P., et al. 2006. J. Pharmacol. Exp. Ther.319, 1376.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable


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