1125758-85-1

1125758-85-1 structure

Name: A 804598
Chemical Name: 2-Cyano-1-[(1S)-1-phenylethyl]-3-(5-quinolinyl)guanidine
CAS Number: 1125758-85-1
Molecular Formula: C₁₉H₁₇N₅
Molecular Weight: 315.37200
Catalog: Signaling Pathways Membrane Transporter/Ion Channel P2X Receptor
Create Date: 2017-02-07 08:51:09
Modify Date: 2024-01-04 13:39:26
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]

Name	2-Cyano-1-[(1S)-1-phenylethyl]-3-(5-quinolinyl)guanidine
Synonyms	N-Cyano-N''-[(1S)-1-phenylethyl]-N'-5-quinolinyl-guanidine A 804598 A-804598

Description	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]
Related Catalog	Signaling Pathways >> Membrane Transporter/Ion Channel >> P2X Receptor Research Areas >> Cancer
References	[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]. Able SL et al. Receptor localization, native tissue binding and ex vivo occupancy for centrally penetrant P2X7 antagonists in the rat. Br J Pharmacol, 2011 Jan, 162(2):405-14.