1、A 839977Cat. No.: HY-13954CAS No.: 870061-27-1Molecular Formula: CHClNOMolecular Weight: 413.26Target: P2X ReceptorPathway: Membrane Transporter/Ion ChannelStorage: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 monthSolvent blocks BzATP-evoked calcium influx at recombinant human, rat a
2、nd 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-1be
3、ta 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 Freunds adjuvant (CFA) (ED50=100 micromol/kg, i.p.) in rats. A-839977 also produced robust antihyperalges
4、ia 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.REFERENCESProduct Data Sheet InhibitorsAgonistsScreening Librarieswww.MedChemE11. Honore P, et al. The antihype
5、ralgesic 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.Caution: Product has not been fully validated for medical applications. For research use only.Tel: 609-228-6898 Fax: 609-228-5909 E-mail: techMedChemEAddress: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USAwww.MedChemE2
