Catalog Number: 3701
Chemical Name: N-[1-[[(Cyanoamino)(5-quinolinylamino)methylene]amino]-2,2-dimethylpropyl]-3,4-dimethoxybenzeneacetamide
Biological Activity
Potent and selective 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. Also reduces neuroblastoma tumor growth in mice.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 20 mM in DMSO
  • Purity:
  • Storage:
    Store at +4°C
  • CAS No:
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.
Background References
  1. 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.
    Honore et al.
    J.Pharmacol.Exp.Ther., 2006;319:1376
  2. Novel P2X7 receptor antagonists ease the pain.
    Br.J.Pharmacol., 2007;151:565
  3. Mammalian P2X7 receptor pharmacology: comparison of recombinant mouse, rat and human P2X7 receptors.
    Donnelly-Roberts et al.
    Br.J.Pharmacol., 2009;157:1203
  4. The P2X7 receptor is a key modulator of the PI3K/GSK3β/VEGF signaling network: evidence in experimental neuroblastoma.
    Amoroso et al.
    Oncogene, 2015;
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