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Introduction of 1125758-85-1 :
A-804598 is a CNS penetrant, competitive and selective P2X7 receptor antagonist with IC50s of 9 nM, 10 nM and 11 nM for mouse, rat and human P2X7 receptors, respectively. IC50 & Target: IC50: 9 nM (mouse P2X7 receptor), 10 nM (rat P2X7 receptor), 11 nM (human P2X7 receptor)In Vitro: Pre-incubation with A-804598 (0.1-10 μM; 1 hour) significantly attenuates BzATP-induced cell loss in a concentration-dependent manner. 3 μM A-804598 exhibits the greatest protective effect against BzATP-induced cytotoxicity. In Vivo: A chroni treatment with A-804598 (intraperitoneal injection; 30 mg/kg; five times a week) decreases the expression of LC3B-II and SQSTM1/p62 in lumbar spinal cord at end stage of disease.