A 839977
Names
Biological Activity
[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].
[Related Catalog]:
[References]
[Related Small Molecules]
Chemical & Physical Properties
[ Molecular Formula ]:
C19H14Cl2N6O
[ Molecular Weight ]:
413.26000
[ Exact Mass ]:
412.06100
[ PSA ]:
80.98000
[ LogP ]:
4.19040