A 839977

Cat. No. 4232

A 839977 C19H14Cl2N6O [870061-27-1]

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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

Soluble to 100 mM in DMSO
>98 %
Store at +4°C

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.

Certificate of Analysis / Safety Data Sheet

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Friedle et al (2010) Recent patents on novel P2X7 receptor antagonists and their potential for reducing central nervous system inflammation. Recent Pat.CNS Drug Discov. 5 35. PMID: 19705995.

Honore et al (2009) The antihyperalgesic activity of a selective P2X7 receptor antagonist, A-839977, is lost in IL-1αβ knockout mice. Behav.Brain.Res. 204 77. PMID: 19464323.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for A 839977 include:

Gangadharan et al (2015) Caveolin-1 regulates P2X7 receptor signaling in osteoblasts. PLoS One 308 C41. PMID: 25318104.

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Keywords: A 839977, supplier, A839977, purinergics, purinoceptors, purines, p2x7, antagonists, antinociceptive, cns, penetrant, Tocris Bioscience, Purinergic (P2X) Receptor Antagonist products

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