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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].

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