A 804598

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]

Signaling Pathways >> Membrane Transporter/Ion Channel >> P2X Receptor

Research Areas >> Cancer

[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.

Adenosine 5'-triphosphate disodium salt | KN-62 | A-740003 | A 438079 | af-353 | AZD9056 hydrochloride | PSB-12062 | A-317491 | A 839977 | Gefapixant | GW791343 | Lappaconitine | CE-224535 | JNJ-54175446