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A 839977

Catalog #: 4232
2 Citations Datasheet / COA / SDS

Discontinued Product

4232 has been discontinued.
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A 839977 | CAS No. 870061-27-1 | P2X Receptor Antagonists
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Description: Potent P2X7 antagonist

Chemical Name: 1-(2,3-Dichlorophenyl)-N-[[2-(2-pyridinyloxy)phenyl]methyl]-1H-tetrazol-5-amine

Purity: ≥98%

Product Details
Citations (2)
Reviews
Biological Activity Technical Data Background Product Datasheets Calculators

Biological Activity

A 839977 is a 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:
413.26
Formula:
C19H14Cl2N6O
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥98%
Storage:
Store at +4°C
CAS No:
870061-27-1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. The P2X7 Receptor Primes IL-1? and the NLRP3 Inflammasome in Astrocytes Exposed to Mechanical Strain
    F Albalawi, W Lu, JM Beckel, JC Lim, SA McCaughey, CH Mitchell
    Front Cell Neurosci, 2017;11(0):227.
  2. MicroRNA-125b regulates microglia activation and motor neuron death in ALS.
    Parisi C, Napoli G, Amadio S, Spalloni A, Apolloni S, Longone P, Volonte C
    Cell Death Differ, 2015;23(3):531-41.
  3. 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
  4. 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

Product Datasheets

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Citations for A 839977

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

2 Citations: Showing 1 - 2

  1. Polarized Cytokine Release Triggered by P2X7 Receptor from Retinal Pigmented Epithelial Cells Dependent on Calcium Influx.
    Authors: Wennan Et al.
    Cells  2020;9
  2. Caveolin-1 regulates P2X7 receptor signaling in osteoblasts.
    Authors: Gangadharan Et al.
    PLoS One  2015;308:C41

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