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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:200 mg
市场价:10286元

产品介绍

产品描述

A 839977 is a P2X7 selective antagonist and the antihyperalgesic effects of P2X7 receptor blockade are mediated by blocking the release of IL-1beta[1]. It blocks BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors (IC50 values are 20 nM, 42 nM and 150 nM respectively) and reduces inflammatory and neuropathic pain in animal models.

体外活性

A 839977 selectively blocks BzATP-evoked calcium influx at mammalian P2X7 receptors, (IC50=20-150 nM), which blocks agonist-evoked YO-PRO uptake and IL-1beta release from differentiated human THP-1 cells. A 839977 (50 nM, pre-treatment 1 hour) significantly prevents pressure-induced rise of IL-1β priming in optic nerve astrocytes[2] and it has been shown to reduce inflammatory and neuropathic pain in animal models[1].

体内活性

A 839977 (30 μmol/kg, 100 μmol/kg, 300 μmol/kg; pre-injected 30mins) dose-dependently reduces thermal hyperalgesia produced by intraplantar administration of complete Freund's adjuvant (CFA) in rats[1] and it attenuates dorsal horn neuronal responses in cancer bearing animals[3]. A 839977 (10 μmol/kg, 30 μmol/kg, 100 μmol/kg; pre-injected 30mins) produces robust antihyperalgesia in the CFA model of inflammatory pain in wild-type mice, but it has no effect on IL-1alphabeta knockout mice[1].

Cas No.

870061-27-1

分子式

C19H14Cl2N6O

分子量

413.26

别名

A 839977

储存和溶解度

DMSO:100 mg/mL (241.98 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years