AZ 10606120 dihydrochloride

Name: AZ 10606120 dihydrochloride
Brand: Tocris Bioscience
SKU: 3323

Tocris Bioscience a Bio-Techne Brand

Catalog # 3323

Citations (15)

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Key Product Details

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)
Molecular Weight:	495.48

View Full Technical Details for AZ 10606120 dihydrochloride

Biological Activity for AZ 10606120 dihydrochloride

AZ 10606120 dihydrochloride is a potent P2X₇ receptor antagonist (K_D 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 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.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.02 mL	10.09 mL	20.18 mL
5 mM	0.40 mL	2.02 mL	4.04 mL
10 mM	0.20 mL	1.01 mL	2.02 mL
50 mM	0.04 mL	0.20 mL	0.40 mL

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References for AZ 10606120 dihydrochloride

References are publications that support the biological activity of the product.

Adinolfi Expression of P2X7 receptor increases in vivo tumor growth. Cancer Res. 2012 PMID: 22505653
Michel Negative and positive allosteric modulators of the P2X₇ receptor. Br.J.Pharmacol. 2008 PMID: 18071294
Michel Direct labelling of the human P2X₇ receptor and identification of positive and negative cooperativity of binding. Br.J.Pharmacol. 2007 PMID: 17339830
Michel and Fonfria Agonist potency at P2X₇ receptors is modulated by structurally diverse lipids. Br.J.Pharmacol. 2007 PMID: 17700717

Citations for AZ 10606120 dihydrochloride (15)

Showing 1 - 10 of 15 citations Showing All

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Citations are publications that use Bio-Techne products. Selected citations for AZ 10606120 dihydrochloride include:

Palygin et al. (2018) Characterization of purinergic receptor expression in ARPKD cystic epithelia. Purinergic Signal. 14:485
PMID: 30417216
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(1)
PMID: 28389651
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
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
Martin et al. (2014) IKKα negatively regulates ASC-dependent inflammasome activation. Nat Commun. 5:4977
PMID: 25266676
Bhaskaracharya et al. (2014) Probenecid blocks human P2X7 receptor-induced dye uptake via a pannexin-1 independent mechanism. PLoS One. 9:e93058
PMID: 24671093
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
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
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
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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