Catalog Number: 3323
Chemical Name: N-[2-[[2-[(2-Hydroxyethyl)amino]ethyl]amino]-5-quinolinyl]-2-tricyclo[3.3.1.13,7]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:
    495.48
  • Formula:
    C25H34N4O2.2HCl
  • Solubility:
    Soluble to 25 mM in water and to 100 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Desiccate at RT
  • CAS No:
    607378-18-7
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
Citations:

The citations listed below are publications that use Tocris products. Selected citations for AZ 10606120 dihydrochloride include:

10 Citations: Showing 1 - 10
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  1. Unique residues in the ATP gated human P2X7 receptor define a novel allosteric binding pocket for the selective antagonist AZ10606120
    Authors: Allsopp
    Sci Rep 2017;7(1)
  2. Neutrophil P2X7 receptors mediate NLRP3 inflammasome-dependent IL-1β secretion in response to ATP.
    Authors: Karmakar Et al.
    Nat.Commun. 2016;7:10555
  3. Active Caspase-1 Induces Plasma Membrane Pores That Precede Pyroptotic Lysis and Are Blocked by Lanthanides
    Authors: Russo Et al.
    The Journal of Immunology 2016;197:1353
  4. The P2X7 receptor regulates cell survival, migration and invasion of pancreatic ductal adenocarcinoma cells.
    Authors: Giannuzzo Et al.
    Purinergic Signal 2015;14:203
  5. Bile acid effects are mediated by ATP release and purinergic signalling in exocrine pancreatic cells.
    Authors: Kowal Et al.
    Mol Cancer 2015;13:28
  6. IKKα negatively regulates ASC-dependent inflammasome activation.
    Authors: Martin Et al.
    Nat Commun 2014;5:4977
  7. P2X7 receptor activation mediates organic cation uptake into human myeloid leukaemic KG-1 cells.
    Authors: Gadeock Et al.
    Mol Biol Cell 2012;8:669
  8. Positive allosteric modulation by ivermectin of human but not murine P2X7 receptors.
    Authors: Nörenberg Et al.
    Br J Pharmacol 2012;167:48
  9. K+ depolarization evokes ATP, adenosine and glutamate release from glia in rat hippocampus: a microelectrode biosensor study.
    Authors: Heinrich Et al.
    Br J Pharmacol 2012;167:1003
  10. Lack of neuroprotection in the absence of P2X7 receptors in toxin-induced animal models of Parkinson's disease.
    Authors: Hracskó Et al.
    Mol Neurodegener 2011;6:28

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