A-804598是一个强的，竞争性，和选择性的P2X7受体拮抗剂，在大鼠，小鼠和体内的IC50分别是10 nM, 9 nM 和11 nM。

＞98%

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

A 804598; A-804598

DMSO: ≥ 32 mg/mL

rat P2X7R ,rat P2X7R ,human P2X7R

A-804598 represents a structurally novel, competitive, and selective antagonist that has equivalent high affinity at rat (IC50 = 10 nM), mouse (IC50 = 9 nM) and human (IC50 = 11 nM) P2X7 receptors. A-804598 also potently blocks agonist stimulated release of IL-1β(IC50 of 8.5 nM) and Yo-Pro uptake (IC50 of 8.1 nM) from differentiated THP-1 cells that natively express human P2X7 receptors. Although A-840598 potently blocks P2X7 receptor activation, at concentrations up to 100 μM, it does not significantly reduce agonist-evoked changes in intracellular calcium concentrations mediated by a variety of other P2X and P2Y receptors. A-840598 shows weak or no activity for interating with a large array of G-protein-coupled receptors, enzymes, transporters, and ion channels (CEREP, Poitiers, France)(IC50 > 5-10 μM).

Inhibition of P2X7 through the antagonist A-804598 in SOD1-G93A mice suppresses SQSTM1/p62 up-regulation in lumbar spinal cord.