AZ 10606120 dihydrochloride
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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%
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
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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. -
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. -
Expression of P2X7 receptor increases in vivo tumor growth.
Adinolfi et al.
Cancer Res., 2012;72:2957 -
Negative and positive allosteric modulators of the P2X7 receptor.
Michel et al.
Br.J.Pharmacol., 2008;153:737 -
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 -
Agonist potency at P2X7 receptors is modulated by structurally diverse lipids.
Michel and Fonfria
Br.J.Pharmacol., 2007;152:523
Product Datasheets
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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
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Characterization of purinergic receptor expression in ARPKD cystic epithelia.
Authors: Palygin Et al.
Purinergic Signal 2018;14:485
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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)
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Neutrophil P2X7 receptors mediate NLRP3 inflammasome-dependent IL-1β secretion in response to ATP.
Authors: Karmakar Et al.
Nat.Commun. 2016;7:10555
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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
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Selected ginsenosides of the protopanaxdiol series are novel positive allosteric modulators of P2X7 receptors.
Authors: Helliwell Et al.
Br J Pharmacol 2015;172:3326
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The P2X7 receptor regulates cell survival, migration and invasion of pancreatic ductal adenocarcinoma cells.
Authors: Giannuzzo Et al.
Purinergic Signal 2015;14:203
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Bile acid effects are mediated by ATP release and purinergic signalling in exocrine pancreatic cells.
Authors: Kowal Et al.
Mol Cancer 2015;13:28
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Probenecid blocks human P2X7 receptor-induced dye uptake via a pannexin-1 independent mechanism.
Authors: Bhaskaracharya Et al.
PLoS One 2014;9:e93058
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IKKα negatively regulates ASC-dependent inflammasome activation.
Authors: Martin Et al.
Nat Commun 2014;5:4977
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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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Natural compounds with P2X7 receptor-modulating properties.
Authors: Fischer Et al.
Purinergic Signal 2013;10:313
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P2X7 receptor activation mediates organic cation uptake into human myeloid leukaemic KG-1 cells.
Authors: Gadeock Et al.
Mol Biol Cell 2012;8:669
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Positive allosteric modulation by iverm. of human but not murine P2X7 receptors.
Authors: Nörenberg Et al.
Br J Pharmacol 2012;167:48
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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
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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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