GSK1370319A - CAS 1001389-31-6

GSK1370319A is a potent P2X7 antagonist (IC50 = 3.2 nM) . GSK1370319A inhibits ATP-induced increase in IL-1β release and caspase 1 activation in lipopolysaccharide (LPS) -primed mixed glia by blocking assembly of the inflammasome in a pannexin 1-dependent manner. GSK1370319A also inhibits ATP-induced subregion-specific neuronal loss in hippocampal organotypic slice cultures, which is dependent on its ability to prevent inflammasome assembly in glia. Significantly, GSK1370319A attenuates age-related deficits in long-term potentiation (LTP) and inhibits the accompanying age-related caspase 1 activity. We conclude that inhibiting P2X (7) receptor-activated NLRP3 inflammasome formation and the consequent IL-1β release from glia preserve neuronal viability and synaptic activity.

Others

Others

1001352

C13H14Cl2N2O2

301.17

C(NCC1=C(Cl)C=C(Cl)C=C1)(=O)[C@H]2N(C)C(=O)CC2

-20°C

Ice Packs

Small Compound