A804598 是一个 CNS 渗透，竞争性和选择性的P2X7受体拮抗剂，作用于小鼠、大鼠和人的 P2X7 受体，IC50s 分别是 9、10 和 11 nM。

A-804598 is a competitive and selective P2X7 receptor antagonist (IC50: 10 nM, rat; 9 nM, mouse; 11 nM, human).

A-804598 effectively blocked IL-1β release in the THP-1 cells (IC50: 8.5 nM). It also blocked agonist-evoked pore formation in differentiated human THP-1 cells (IC50: 8.1 nM) with similar potency as in the calcium-influx assay. [1]

According to the autoradiographic analysis of coronal rat brain sections, there was specific binding of [3H]-A-804598 throughout the rat brain. In the grey matter of the L4-L6 region of the rat spinal cord, it was also found that high levels of [3H]-A-804598 specific binding. [2]

1125758-85-1

C19H17N5

315.38

A 804598

DMSO:31.5 mg/mL(100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years