A-804598 is a competitive, and selective P2X7 receptor antagonist with IC50 of 10 nM, 9 nM and 11 nM in rat, mouse and human P2X7 receptors respectively.
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描述 | A-804598 effectively crosses into the central nervous system and acts as a competitive inhibitor, selectively targeting P2X7 receptors. It demonstrates IC50 values of 9 nM for mice, 10 nM for rats, and 11 nM for humans, showcasing its efficacy across these species' P2X7 receptors[1]. Treating cells with A-804598 at concentrations ranging from 0.1 to 10 μM for one hour markedly reduces cell death caused by BzATP in a dose-dependent fashion. The most substantial protective effect against the cytotoxicity triggered by BzATP is observed at a concentration of 3 μM A-804598[2]. |
作用机制 | A-804598 can competitively bind to P2X7 receptor.[1] |
Dose | Mice: 90 mg/kg[2] (i.p.) Rat: 3 mg/kg - 30 mg/kg[3] (i.p.) |
Administration | i.p. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
3.17mL 0.63mL 0.32mL |
15.85mL 3.17mL 1.59mL |
31.71mL 6.34mL 3.17mL |
CAS号 | 1125758-85-1 |
分子式 | C19H17N5 |
分子量 | 315.37 |
SMILES Code | C[C@H](N/C(NC1=C2C=CC=NC2=CC=C1)=N/C#N)C3=CC=CC=C3 |
MDL No. | MFCD22683834 |
别名 | |
运输 | 蓝冰 |
InChI Key | PQYCRDPLPKGSME-AWEZNQCLSA-N |
Pubchem ID | 53325874 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Keep in dark place, sealed in dry, 2-8°C |
溶解方案 |
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动物实验配方 |
IP 5%DMSO+ 30%PEG+2% tween80 +H2O 6 mg/mL clear |