A-804598

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

A-804598 是一种竞争性、选择性 P2X7 受体拮抗剂（IC50：10 nM，大鼠；9 nM，小鼠；11 nM，人）。

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

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.

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 weekResult:Decreased SQSTM1/p62 expression.

A-804598 | A 804598 | A804598.

Metabolic Enzyme/Protease

MAO

P2X7

Cancer

——

1125758-85-1

315.37

C19H17N5

>98% (HPLC)

DMSO : ≥ 32 mg/mL 101.47 mM

C[C@@H](c1ccccc1)N=C(NC#N)Nc1cccc2c1cccn2

N-Cyano-N′′-[(1S)-1-phenylethyl]-N′-5-quinolinyl-guanidine

(-20℃)

With Ice Pack

≥ 2 years