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.
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.
Cell Cytotoxicity Assay
Cell Line:
microglial cell
Concentration:
0.1, 0.3, 1, 3, 10 μM
Incubation Time:
1 hour
Result:
Protected against BzATP-induced cytotoxicity in both inactivated and activated microglia.
体内研究
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.
Animal Model:
Adult B6.Cg-Tg (SOD1-G93A) 1Gur/J female mice
Dosage:
30 mg/kg
Administration:
Intraperitoneal injection; five times a week
Result:
Decreased SQSTM1/p62 expression.
分子式
C19H17N5
分子量
315.37
CAS号
1125758-85-1
运输条件
Room temperature in continental US; may vary elsewhere.