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A 804598

Catalog No.
P2X7 antagonist,potent and selective
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A 804598 is a potent and selective antagonist of P2X7 receptor with IC50 values of 8.9, 9.9 and 10.9 nM for mouse, rat and human P2X7 receptors, respectively [1].

P2X purinoceptor 7 (P2X7 receptor) is a purinoceptor and is activated by high concentrations of ATP. P2X7 receptor plays an important role in ATP-mediated cell death, inflammation and regulation of receptor trafficking.

A 804598 is a potent and selective P2X7 receptor antagonist. In differentiated THP-1 cells that expressed human P2X7 receptors, A 804598 inhibited BzATP stimulated Yo-Pro uptake and release of IL-1β. In 1321N1 cells expressed recombinant rat P2X7 receptor, A 804598 showed high affinity with Kd = 2.4 nM [1]. A 804598 inhibited BZ-ATP stimulated calcium influx with IC50 value of 28.71 nM in a concentration-dependent way. A-804598 was a potent P2X7 receptor antagonist with Ki value of 7.51 nM [2].

In adult male rats, footshock increased the mRNA levels of CD14 and IL-1β in the paraventricular nucleus. While A-804598 (25 mg/kg) partially inhibited these effects [3].

[1].  Donnelly-Roberts DL, Namovic MT, Surber B, et al. [3H]A-804598 ([3H]2-cyano-1-[(1S)-1-phenylethyl]-3-quinolin-5-ylguanidine) is a novel, potent, and selective antagonist radioligand for P2X7 receptors. Neuropharmacology, 2009, 56(1): 223-229.
[2].  Able SL, Fish RL, Bye H, et al. Receptor localization, native tissue binding and ex vivo occupancy for centrally penetrant P2X7 antagonists in the rat. Br J Pharmacol. 2011, 162(2): 405-414.
[3].  Catanzaro JM1, Hueston CM, Deak MM, et al. The impact of the P2X7 receptor antagonist A-804598 on neuroimmune and behavioral consequences of stress. Behav Pharmacol, 2014, 25(5-6): 582-598.

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
Cas No.1125758-85-1
SolubilitySoluble in DMSO
SDFDownload SDF
Canonical SMILESN#CN/C(NC1=C2C(N=CC=C2)=CC=C1)=N\[[email protected]@H](C)C3=CC=CC=C3
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

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