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A 740003

Cat. No. 3701

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Chemical Name: N-[1-[[(Cyanoamino)(5-quinolinylamino)methylene]amino]-2,2-dimethylpropyl]-3,4-dimethoxybenzeneacetamide

Biological Activity

Potent, selective and competitive P2X₇ receptor antagonist (IC₅₀ values are 18 and 40 nM for rat and human receptors respectively). Displays selectivity over a variety of P2X and P2Y receptors up to a concentration of 100 μM. Reduces nociception in animal models of persistent neuropathic and inflammatory pain.

Technical Data

M.Wt:

474.55

Formula:

C₂₆H₃₀N₆O₃

Solubility:

Soluble to 100 mM in DMSO

Purity:

>98 %

Storage:

Store at +4°C

CAS No:

861393-28-4

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

Honore et al (2006) A-740003 [N-(1-{[(cyanoimino)(5-quinolinylamino)methyl]amino}-2,2-dimethylpropyl)-2-(3,4-dimethoxyphenyl)acetamide], a novel and selective P2X₇ receptor antagonist, dose-dependently reduces neuropathic pain in the rat. J.Pharmacol.Exp.Ther. 319 1376. PMID: 16982702.

King (2007) Novel P2X₇ receptor antagonists ease the pain. Br.J.Pharmacol. 151 565. PMID: 17471176.

Donnelly-Roberts et al (2009) Mammalian P2X7 receptor pharmacology: comparison of recombinant mouse, rat and human P2X7 receptors. Br.J.Pharmacol. 157 1203. PMID: 19558545.

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