Catalog Number: 3323
Chemical Name: N-[2-[[2-[(2-Hydroxyethyl)amino]ethyl]amino]-5-quinolinyl]-2-tricyclo[,7]dec-1-ylacetamide dihydrochloride
Biological Activity
Potent P2X7 receptor antagonist (KD values are 1.4 and 19 nM at human and rat P2X7 receptors respectively). Binds in a positive cooperative manner to sites distinct from, but coupled to, the ATP binding site and acts as a negative allosteric modulator. Inhibits tumor growth and displays antiangiogenic effects in mice.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 25 mM in water and to 100 mM in DMSO
  • Purity:
  • Storage:
    Desiccate at RT
  • 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.
Additional Information
Licensing Caveats:
Sold for research purposes under agreement from AstraZeneca
Background References
  1. Negative and positive allosteric modulators of the P2X7 receptor.
    Michel et al.
    Br.J.Pharmacol., 2008;153:737
  2. Direct labelling of the human P2X7 receptor and identification of positive and negative cooperativity of binding.
    Michel et al.
    Br.J.Pharmacol., 2007;151:103
  3. Agonist potency at P2X7 receptors is modulated by structurally diverse lipids.
    Michel and Fonfria
    Br.J.Pharmacol., 2007;152:523
  4. Expression of P2X7 receptor increases in vivo tumor growth.
    Adinolfi et al.
    Cancer Res., 2012;72:2957
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