A 804598
Chemical Name: N-Cyano-N"-[(1S)-1-phenylethyl]-N'-5-quinolinyl-guanidine
Purity: ≥99%
Biological Activity
A 804598 is a potent, 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).Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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[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.
Donnelly-Roberts et al.
Neuropharmacology, 2009;56:223 -
Receptor localization, native tissue binding and ex vivo occupancy for centrally penetrant P2X7 antagonists in the rat.
Able et al.
Br.J.Pharmacol., 2011;162:405
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Citations for A 804598
The citations listed below are publications that use Tocris products. Selected citations for A 804598 include:
2 Citations: Showing 1 - 2
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Connexin-43-dependent ATP release mediates macrophage activation during sepsis.
Authors: Dosch Et al.
Elife 2019;8
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A novel mechanism of autophagic cell death in dystrophic muscle regulated by P2RX7 receptor large-pore formation and HSP90.
Authors: Young Et al.
Cell Commun Signal 2015;11:113
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RAW macrophages were stimulated with LPS (200 ng/ml) in the absence or presence of A 804598 (1 μM) or MRS 2578 (100 μM) for 8 h to follow iNOS expression by qPCR. Both compounds inhibited LPS-induced iNOS expression revealing role of purinergic receptors.
