AZ 10606120 dihydrochloride

Cat. No. 3323

AZ 10606120 dihydrochloride C25H34N4O2.2HCl [607378-18-7]

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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.

Licensing Information

Sold for research purposes under agreement from AstraZeneca

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.

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch
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Safety Data Sheet: View Safety Data Sheet

Adinolfi et al (2012) Expression of P2X7 receptor increases in vivo tumor growth. Cancer Res. 72 2957. PMID: 22505653.

Michel et al (2008) Negative and positive allosteric modulators of the P2X7 receptor. Br.J.Pharmacol. 153 737. PMID: 18071294.

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.

If you know of a relevant reference for this product please let us know.

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.

Martin et al (2014) IKKα negatively regulates ASC-dependent inflammasome activation. Nat Commun 5 4977. PMID: 25266676.

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.

Nörenberg et al (2012) Positive allosteric modulation by ivermectin of human but not murine P2X7 receptors. Br J Pharmacol 167 48. PMID: 22506590.

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.

Do you know of a great paper that uses AZ 10606120 dihydrochloride from Tocris? If so please let us know.show all ▼show less ▲

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Keywords: AZ 10606120 dihydrochloride, supplier, Potent, P2X7, receptor, antagonists, Receptors, Purinergic, purinoceptors, AZ10606120, dihydrochloride, AstraZeneca, Tocris Bioscience, Purinergic (P2X) Receptor Antagonist products

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