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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.
Sold for research purposes under agreement from AstraZeneca
AZ 10606120 dihydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
|Storage||Desiccate at RT|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
The following data is based on the product molecular weight 495.48. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.02 mL||10.09 mL||20.18 mL|
|5 mM||0.4 mL||2.02 mL||4.04 mL|
|10 mM||0.2 mL||1.01 mL||2.02 mL|
|50 mM||0.04 mL||0.2 mL||0.4 mL|
References are publications that support the biological activity of the product.
Michel et al (2007) Direct labelling of the human P2X7 receptor and identification of positive and negative cooperativity of binding. Br.J.Pharmacol. 151 103 PMID: 17339830
Michel and Fonfria (2007) Agonist potency at P2X7 receptors is modulated by structurally diverse lipids. Br.J.Pharmacol. 152 523 PMID: 17700717
Michel et al (2008) Negative and positive allosteric modulators of the P2X7 receptor. Br.J.Pharmacol. 153 737 PMID: 18071294
Adinolfi et al (2012) Expression of P2X7 receptor increases in vivo tumor growth. Cancer Res. 72 2957 PMID: 22505653
If you know of a relevant reference for AZ 10606120 dihydrochloride, please let us know.
Keywords: AZ 10606120 dihydrochloride, AZ 10606120 dihydrochloride supplier, Potent, P2X7, receptor, antagonists, Receptors, Purinergic, purinoceptors, AZ10606120, dihydrochloride, AstraZeneca, P2X, 3323, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for AZ 10606120 dihydrochloride include:
Karmakar et al (2016) Neutrophil P2X7 receptors mediate NLRP3 inflammasome-dependent IL-1β secretion in response to ATP. Nat.Commun. 7 10555 PMID: 26877061
Russo et al (2016) Active Caspase-1 Induces Plasma Membrane Pores That Precede Pyroptotic Lysis and Are Blocked by Lanthanides The Journal of Immunology 197 1353 PMID: 27385778
Kowal et al (2015) Bile acid effects are mediated by ATP release and purinergic signalling in exocrine pancreatic cells. Mol Cancer 13 28 PMID: 26050734
Giannuzzo et al (2015) The P2X7 receptor regulates cell survival, migration and invasion of pancreatic ductal adenocarcinoma cells. Purinergic Signal 14 203 PMID: 26607222
Martin et al (2014) IKKα negatively regulates ASC-dependent inflammasome activation. Nat Commun 5 4977 PMID: 25266676
Kaiser et al (2014) Tanshinone II A sulfonate, but not tanshinone II A, acts as potent negative allosteric modulator of the human purinergic receptor P2X7. J Pharmacol Exp Ther 350 531 PMID: 24970925
Bhaskaracharya et al (2014) Probenecid blocks human P2X7 receptor-induced dye uptake via a pannexin-1 independent mechanism. PLoS One 9 e93058 PMID: 24671093
Gadeock et al (2012) P2X7 receptor activation mediates organic cation uptake into human myeloid leukaemic KG-1 cells. Mol Biol Cell 8 669 PMID: 22661222
Fischer et al (2013) Natural compounds with P2X7 receptor-modulating properties. Purinergic Signal 10 313 PMID: 24163006
Nörenberg et al (2012) Positive allosteric modulation by iverm. of human but not murine P2X7 receptors. Br J Pharmacol 167 48 PMID: 22506590
Heinrich et al (2012) K+ depolarization evokes ATP, adenosine and glutamate release from glia in rat hippocampus: a microelectrode biosensor study. Br J Pharmacol 167 1003 PMID: 22394324
Allsopp (2017) Unique residues in the ATP gated human P2X7 receptor define a novel allosteric binding pocket for the selective antagonist AZ10606120 Sci Rep 7 PMID: 28389651
Helliwell et al (2015) Selected ginsenosides of the protopanaxdiol series are novel positive allosteric modulators of P2X7 receptors. Br J Pharmacol 172 3326 PMID: 25752193
Palygin et al (2018) Characterization of purinergic receptor expression in ARPKD cystic epithelia. Purinergic Signal 14 485 PMID: 30417216
Hracskó et al (2011) Lack of neuroprotection in the absence of P2X7 receptors in toxin-induced animal models of Parkinson's disease. Mol Neurodegener 6 28 PMID: 21542899
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Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.