A 839977

A 839977 is a P2X7 selective antagonist; 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; the antihyperalgesic effects of P2X7 receptor blockade are mediated by blocking the release of IL-1beta[1].


Cat. No.: EX-A14522	Purity: >98%

	Chemical structure of A 839977

For research only, Do not use for Human!

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CAS No.	870061-27-1
Purity	>98%
Formula	C19H14Cl2N6O
Mol Weight	413.26
Color	White to off-white
State	Solid
Solubility	soluble in DMSO
Shelf Life	>3 years if stored properly
Storage	Powder -20℃, 3 years; 4℃, 2 years; In solvent -20℃, 1 year;
Shipping	Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Reference:	[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-1β 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.
CoA	CoA of A 839977

Smiles:	C1=CC=C(C(=C1)CNC2=NN=NN2C3=C(C(=CC=C3)Cl)Cl)OC4=CC=CC=N4


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