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% (HPLC)
Datasheet
Citations (15)
Reviews
Literature (1)

Biological Activity for AZ 10606120 dihydrochloride

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.

Licensing Information

Sold for research purposes under agreement from AstraZeneca

Compound Libraries for AZ 10606120 dihydrochloride

AZ 10606120 dihydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for AZ 10606120 dihydrochloride

M. Wt 495.48
Formula C25H34N4O2.2HCl
Storage Desiccate at RT
Purity ≥98% (HPLC)
CAS Number 607378-18-7
PubChem ID 56972227
InChI Key BVFONFUUWORSPO-UHFFFAOYSA-N
Smiles O=C(NC4=C(C=CC(NCCNCCO)=N5)C5=CC=C4)CC1(C3)CC2CC(CC3C2)C1.Cl.Cl

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.

Solubility Data for AZ 10606120 dihydrochloride

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 12.39 25
DMSO 49.55 100

Preparing Stock Solutions for AZ 10606120 dihydrochloride

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.

Select a batch to recalculate based on the batch molecular weight:
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

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Product Datasheets for AZ 10606120 dihydrochloride

Certificate of Analysis / Product Datasheet
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References for AZ 10606120 dihydrochloride

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


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Keywords: AZ 10606120 dihydrochloride, AZ 10606120 dihydrochloride supplier, Potent, P2X7, receptor, antagonists, Receptors, Purinergic, purinoceptors, AZ10606120, dihydrochloride, AstraZeneca, P2X, 3323, Tocris Bioscience

15 Citations for AZ 10606120 dihydrochloride

Citations are publications that use Tocris products. Selected citations for AZ 10606120 dihydrochloride include:

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

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

Palygin et al (2018) Characterization of purinergic receptor expression in ARPKD cystic epithelia. Purinergic Signal 14 485 PMID: 30417216

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

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

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

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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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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P2X and P2Y Receptors Scientific Review

P2X and P2Y Receptors Scientific Review

Written by Kenneth Jacobson, this review provides an overview of the different subtypes and structures of the P2 receptor families, as well as the pharmacological probes used to study them; compounds available from Tocris are listed.