Chemical Name: N-Cyano-N"-[(1S)-1-phenylethyl]-N'-5-quinolinyl-guanidine
Biological ActivityA 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).
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Tocris products are intended for laboratory research use only, unless stated otherwise.
[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.
Receptor localization, native tissue binding and ex vivo occupancy for centrally penetrant P2X7 antagonists in the rat.
Able et al.
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
Connexin-43-dependent ATP release mediates macrophage activation during sepsis.
Authors: Dosch Et al.
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.