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A 839977
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
A 839977图片
CAS NO:870061-27-1
包装与价格：
包装价格(元)
10mg电议
50mg电议

产品介绍
A 839977 是 P2X7 选择性拮抗剂；它在重组人、大鼠和小鼠 P2X7 受体处阻断 BzATP 诱发的钙流入（IC50 值分别为 20 nM、42 nM 和 150 nM）并减少动物模型中的炎症和神经性疼痛； P2X7受体阻断的抗痛觉过敏作用是通过阻断IL-1beta的释放来介导的。
Cas No.870061-27-1
化学名(E)-N-(1-(2,3-dichlorophenyl)-1H-tetrazol-5(2H)-ylidene)-1-(2-(pyridin-2-yloxy)phenyl)methanamine
Canonical SMILESClC1=C(Cl)C(N2/C(N=NN2)=N\CC3=CC=CC=C3OC4=CC=CC=N4)=CC=C1
分子式C19H14Cl2N6O
分子量413.26
溶解度Soluble in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

A839977 is a novel and selective antagonist of P2X7 receptor with the IC50 values of 20 nM, 42nM and 150nM for human, rat and mouse, respectively [1].

A839977 has been reported to block BzATP-evoked changes in intracellular calcium concentrations in 132N1 cells stable expressing P2X7 receptors with the IC50 values of 20 nM, 42nM and 150nM for human, rat and mouse, respectively. In addition, A839977 has also revealed to inhibit BzATP-stimulated IL-1β release and YO-PRO uptake with the IC50 of 37nM and 7nM, respectively, in differentiated human THP-1 cells. Besides, A839977 has been noted to produce parallel rightward shifts in BzATP concentration-effect calcium influx curves with the pAα value of 8.1. Apart from these, A839977 has been exhibited to reduce CFA-induced thermal hyperalgesia in a dose-dependent fashion with the ED50 value of 100μmol/kg(i.p.) [1].

References:
[1] Honore P1, Donnelly-Roberts D, Namovic M, Zhong C, Wade C, Chandran P, Zhu C, Carroll W, Perez-Medrano A, Iwakura Y, Jarvis MF. The antihyperalgesic activity of a selective P2X7 receptor antagonist, A-839977, is lost in IL-1alphabeta knockout mice. Behav Brain Res. 2009 Dec 1;204(1):77-81.