A-804598

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Chemical Structure| 1125758-85-1 同义名 : -
CAS号 : 1125758-85-1
货号 : A270115
分子式 : C19H17N5
纯度 : 99%+
分子量 : 315.372
MDL号 : MFCD22683834
存储条件：

Pure form Keep in dark place,Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(95.13 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

IP 5%DMSO+ 30%PEG+2% tween80 +H2O 6 mg/mL clear

生物活性
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].
实验方案
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
参考文献

[1]Donnelly-Roberts DL et al. [3H]A-804598 ([3H]2-cyano-1-[(1S)-1-phenylethyl]-3-quinolin-5-ylguanidine) is a novel, potent, and selective antagonist radioligand for P2X7 receptors. Neuropharmacology, 2009 Jan, 56(1):223-9.

[2]Yingbo He et al. The role of microglial P2X7: modulation of cell death and cytokine release. Neuroinflammation, 2017 Jul, 14(1):135.

[3]Paola Fabbrizio et al. P2X7 Receptor Activation Modulates Autophagy in SOD1-G93A Mouse Microglia.Cell Neurosci, 2017 Aug, 11:249.