TargetMol

A 839977

Product Code:
 
TAR-T14076
Product Group:
 
Inhibitors and Activators
Supplier:
 
TargetMol
Regulatory Status:
 
RUO
Shipping:
 
cool pack
Storage:
 
-20℃
1 / 1
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Further Information

Bioactivity:
A 839977 is a P2X7 selective antagonist and the antihyperalgesic effects of P2X7 receptor blockade are mediated by blocking the release of IL-1beta[1]. It blocks BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors (IC50 values are 20 nM, 42 nM and 150 nM respectively) and reduces inflammatory and neuropathic pain in animal models.
CAS:
870061-27-1
Formula:
C19H14Cl2N6O
Molecular Weight:
413.26
Purity:
0.98
SMILES:
Clc1cccc(c1Cl)-n1nnnc1NCc1ccccc1Oc1ccccn1

References

1. Honore P, et al. The antihyperalgesic 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. 2. Albalawi F et.al, The P2X7 Receptor Primes IL-1? and the NLRP3 Inflammasome in Astrocytes Exposed to Mechanical Strain. Front Cell Neurosci. 2017 Aug 8;11:227 3. Falk S et al.P2X7 receptor-mediated analgesia in cancer-induced bone pain. Neuroscience. 2015 Apr 16; 291:93-105.