Home / P2X Receptor Antagonists / AZ 10606120 dihydrochloride

AZ 10606120 dihydrochloride

Catalog #: 3323
15 Citations Datasheet / COA / SDS
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3323/10
3323/50
AZ 10606120 dihydrochloride | CAS No. 607378-18-7 | P2X Receptor Antagonists
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Description: Potent P2X7 antagonist

Chemical Name: N-[2-[[2-[(2-Hydroxyethyl)amino]ethyl]amino]-5-quinolinyl]-2-tricyclo[3.3.1.13,7]dec-1-ylacetamide dihydrochloride

Purity: ≥98%

Product Details
Citations (15)
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Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

AZ 10606120 dihydrochloride is a 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Licensing Caveats:
Sold for research purposes under agreement from AstraZeneca

Background References

  1. Human beta Defensin-3 Increases CD86 Expression on Monocytes by Activating the ATP-Gated Channel P2X7.
    Lioi A, Ferrari B, Dubyak G, Weinberg A, Sieg S
    J Immunol, 2015;195(9):4438-45.
  2. Accelerated tumor progression in mice lacking the ATP receptor P2X7.
    Adinolfi E, Capece M, Franceschini A, Falzoni S, Giuliani A, Rotondo A, Sarti A, Bonora M, Syberg S, Corigliano D, Pinton P, Jorgensen N, Abelli L, Emionite L, Raffaghello L, Pistoia V, Di Virgilio F
    Cancer Res, 2015;75(4):635-44.
  3. Expression of P2X7 receptor increases in vivo tumor growth.
    Adinolfi et al.
    Cancer Res., 2012;72:2957
  4. Negative and positive allosteric modulators of the P2X7 receptor.
    Michel et al.
    Br.J.Pharmacol., 2008;153:737
  5. 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
  6. Agonist potency at P2X7 receptors is modulated by structurally diverse lipids.
    Michel and Fonfria
    Br.J.Pharmacol., 2007;152:523

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Citations for AZ 10606120 dihydrochloride

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

15 Citations: Showing 1 - 10

  1. Characterization of purinergic receptor expression in ARPKD cystic epithelia.
    Authors: Palygin Et al.
    Purinergic Signal  2018;14:485
  2. 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)
  3. Neutrophil P2X7 receptors mediate NLRP3 inflammasome-dependent IL-1β secretion in response to ATP.
    Authors: Karmakar Et al.
    Nat.Commun.  2016;7:10555
  4. 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
  5. Selected ginsenosides of the protopanaxdiol series are novel positive allosteric modulators of P2X7 receptors.
    Authors: Helliwell Et al.
    Br J Pharmacol  2015;172:3326
  6. The P2X7 receptor regulates cell survival, migration and invasion of pancreatic ductal adenocarcinoma cells.
    Authors: Giannuzzo Et al.
    Purinergic Signal  2015;14:203
  7. Bile acid effects are mediated by ATP release and purinergic signalling in exocrine pancreatic cells.
    Authors: Kowal Et al.
    Mol Cancer  2015;13:28
  8. Probenecid blocks human P2X7 receptor-induced dye uptake via a pannexin-1 independent mechanism.
    Authors: Bhaskaracharya Et al.
    PLoS One  2014;9:e93058
  9. IKKα negatively regulates ASC-dependent inflammasome activation.
    Authors: Martin Et al.
    Nat Commun  2014;5:4977
  10. Tanshinone II A sulfonate, but not tanshinone II A, acts as potent negative allosteric modulator of the human purinergic receptor P2X7.
    Authors: Kaiser Et al.
    J Pharmacol Exp Ther  2014;350:531

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