"目錄號: HY-13954
Membrane Transporter/Ion Channel-
A-839977是選擇性P2X7受體拮抗劑瘸恼，能阻斷BzATP激發(fā)的鈣流奥吩，對人橡淑、大小鼠的P2X7受體的IC50分別為20构拳，42和150 nM。
相關(guān)產(chǎn)品
A-740003-KN-62-A 438079 (hydrochloride)-ATP disodium salt-AF-353-A-317491-AZD9056 hydrochloride-A-804598-GW791343 dihydrochloride-PSB-12062-Lappaconitine-
生物活性
Description
A-839977 is a novel and selective P2X7 antagonist; blocks BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors (IC50 values are 20, 42 and 150 nM respectively).IC50 Value: Target: P2X7in vitro: A-839977 potently (IC50=20-150 nM) blocked BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors. A-839977 also potently blocked agonist-evoked YO-PRO uptake and IL-1beta release from differentiated human THP-1 cells [1]. in vivo: Systemic administration of A-839977 dose-dependently reduced thermal hyperalgesia produced by intraplantar administration of complete Freund's adjuvant (CFA) (ED50=100 micromol/kg, i.p.) in rats. A-839977 also produced robust antihyperalgesia in the CFA model of inflammatory pain in wild-type mice (ED50=40 micromol/kg, i.p.), but the antihyperalgesic effects of A-839977 were completely absent in IL-1alphabeta knockout mice [1].
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