GSK-1482160 is a CNS-penetrant negative allosteric modulator of P2X7 receptor with oral activity. The P2X7 receptor is involved in the production of pro-inflammatory cytokines by central and peripheral immune cells, so GSK-1482160 has the potential to study inflammatory diseases. GSK-1482160 shows excellent in vitro potency (in functional and electrophysiological assays at recombinant and naive P2X7 receptors across multiple species including humans) and cross-target selectivity.

98%

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

DMSO:90.0 mg/mL (268.9 mM)

ATP-induced secretion of tau-containing exosome was significantly suppressed by GSK-1482160 treatment from primary murine microglia, but not from neurons or astrocytes [2].

Oral administration of GSK-1482160 significantly reduced accumulation of MC1+ and Alz50+ misfolded tau in hippocampal regions, which was accompanied with reduced accumulation of Tsg101, an exosome marker, in hippocampal neurons. GSK-1482160 also significantly increased accumulation of Tsg101 and CD81 in microglia in vivo, suggesting its suppression of P2RX7-induced exosome secretion from microglia [2].