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A 804598

Cat. No. 4473

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Chemical Name: N-Cyano-N"-[(1S)-1-phenylethyl]-N'-5-quinolinyl-guanidine

Biological Activity

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 (K_{i app} = 2.4 nM for rat P2X₇ receptors).

Technical Data

M.Wt:

315.37

Formula:

C₁₉H₁₇N₅

Solubility:

Soluble to 100 mM in DMSO

Purity:

>99 %

Storage:

Store at -20°C

CAS No:

1125758-85-1

The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.

Resources

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch

Safety Data Sheet: View Safety Data Sheet

References

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.

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.

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