A-804598 is a novel, competitive, and selective P2X7 receptor antagonist with IC50 of 10 nM, 9 nM and 11 nM in rat, mouse and human P2X7 receptors respectively.
A 804598;2-Cyano-1-[(1S)-1-phenylethyl]-3-(5-quinolinyl)guanidine;A-804598;N-Cyano-N′′-[(1S)-1-phenylethyl]-N′-5-quinolinyl-guanidine;A804598;N-cyano-N''-[(1s)-1-phenylethyl]-N'-5-quinolinyl-guanidine;1-cyano-2-[(1S)-1-phenylethyl]-3-quinolin-5-ylguanidine;GTPL4121;AOB1737;HMS3886P12;BCP19303;BDBM50237707;BDBM50298708;s8725;Q27074085;(S)-2-cyano-1-(1-phenylethyl)-3-(quinolin-5-yl)guanidine;1-cyano-2-[(1S)-1-phenylethyl]-3-(quinolin-5-yl)guanidine;1-cyano-2-[(1S)-1-
A-804598 is a novel, competitive, and selective P2X7 receptor antagonist with IC50 of 10 nM, 9 nM and 11 nM in rat, mouse and human P2X7 receptors respectively.
In Vitro
A-804598 potently blocked IL-1β release in the THP-1 cells (IC50 of 8.5 nM). A-804598 also blocked agonist-evoked pore formation in differentiated human THP-1 cells (IC50 of 8.1 nM) with similar potency as in the calcium-influx assay. [1]
In Vivo
Autoradiographic analysis of coronal rat brain sections revealed that there was specific binding of [3H]-A-804598 throughout the rat brain. High levels of [3H]-A-804598 specific binding were also found in the grey matter of the L4-L6 region of the rat spinal cord. [2]
Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.
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