A 839977 (CAS 870061-27-1): R&D Systems
Catalog Number: 4232
Chemical Name: 1-(2,3-Dichlorophenyl)-N-[[2-(2-pyridinyloxy)phenyl]methyl]-1H-tetrazol-5-amine
Biological Activity
Potent P2X7 antagonist; blocks BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors (IC50 values are 20, 42 and 150 nM respectively). Displays antinociceptive effects in rat and mice models of inflammatory pain. CNS penetrant.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
  • Storage:
    Store at +4°C
  • CAS No:
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. The antihyperalgesic activity of a selective P2X7 receptor antagonist, A-839977, is lost in IL-1αβ knockout mice.
    Honore et al.
    Behav.Brain.Res., 2009;204:77
  2. Recent patents on novel P2X7 receptor antagonists and their potential for reducing central nervous system inflammation.
    Friedle et al.
    Recent Pat.CNS Drug Discov., 2010;5:35

The citations listed below are publications that use Tocris products. Selected citations for A 839977 include:

1 Citations: Showing 1 - 1

  1. Caveolin-1 regulates P2X7 receptor signaling in osteoblasts.
    Authors: Gangadharan Et al.
    PLoS One 2015;308:C41

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