Cat. No. 4473
Chemical Name: N-Cyano-N"-[(1S)-1-phenylethyl]-N'-5-
Biological ActivityPotent, competitive P2X7 receptor antagonist (IC50 values are 8.9, 9.9 and 10.9 nM for mouse, rat and human P2X7 receptors respectively). Selective for P2X7 receptors (IC50 > 5-10 μM for a wide array of cell surface receptors and ion channels). Binds with high affinity (Ki app = 2.4 nM for rat P2X7 receptors).
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
Able et al (2011) Receptor localization, native tissue binding and ex vivo occupancy for centrally penetrant P2X7 antagonists in the rat. Br.J.Pharmacol. 162 405. PMID: 20840537.
Donnelly-Roberts et al (2009) [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 56 223. PMID: 18602931.
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Citations are publications that use Tocris products. Selected citations for A 804598 include:
Young et al (2015) A novel mechanism of autophagic cell death in dystrophic muscle regulated by P2RX7 receptor large-pore formation and HSP90. Cell Commun Signal 11 113. PMID: 25700737.
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Keywords: A 804598, supplier, A804598, purinergic, receptors, P2X7, antagonists, inhibitors, inhibits, potent, selective, competitive, high, affinity, Tocris Bioscience, Purinergic (P2X) Receptor Antagonist products