A 740003

Name: A 740003
Brand: Tocris Bioscience
SKU: 3701

Tocris Bioscience a Bio-Techne Brand

Catalog # 3701

Citations (13)

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Key Product Details

Description:	Potent and selective P2X₇ antagonist
Chemical Name:	N-[1-[[(Cyanoamino)(5-quinolinylamino)methylene]amino]-2,2-dimethylpropyl]-3,4-dimethoxybenzeneacetamide
Purity:	≥98% (HPLC)
Molecular Weight:	474.55

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Biological Activity for A 740003

A 740003 is a potent and selective P2X₇ receptor antagonist (IC₅₀ values are 18 and 40 nM for rat and human receptors respectively). Displays selectivity over a variety of P2X and P2Y receptors up to a concentration of 100 μM. Reduces nociception in animal models of persistent neuropathic and inflammatory pain. Also reduces neuroblastoma tumor growth in mice.

Compound Libraries for A 740003

A 740003 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for A 740003

M. Wt	474.55
Formula	C₂₆H₃₀N₆O₃
Storage	Store at +4°C
Purity	≥98% (HPLC)
CAS Number	861393-28-4
PubChem ID	11351968
InChi Key	PUHSRMSFDASMAE-UHFFFAOYSA-N
Smiles	CC(C)(C)C(NC(CC3=CC(OC)=C(OC)C=C3)=O)N/C(NC2=CC=CC1=NC=CC=C12)=N/C#N

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 A 740003

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	9.49	20

Preparing Stock Solutions for A 740003

The following data is based on the product molecular weight 474.55.

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
0.2 mM	10.54 mL	52.68 mL	105.36 mL
1 mM	2.11 mL	10.54 mL	21.07 mL
2 mM	1.05 mL	5.27 mL	10.54 mL
10 mM	0.21 mL	1.05 mL	2.11 mL

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References for A 740003

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

Amoroso The P2X7 receptor is a key modulator of the PI3K/GSK3β/VEGF signaling network: evidence in experimental neuroblastoma. Oncogene 2015 PMID: 25619831
Donnelly-Roberts Mammalian P2X7 receptor pharmacology: comparison of recombinant mouse, rat and human P2X7 receptors. Br.J.Pharmacol. 2009 PMID: 19558545
King Novel P2X₇ receptor antagonists ease the pain. Br.J.Pharmacol. 2007 PMID: 17471176
Honore A-740003 [N-(1-{[(cyanoimino)(5-quinolinylamino)methyl]amino}-2,2-dimethylpropyl)-2-(3,4-dimethoxyphenyl)acetamide], a novel and selective P2X₇ receptor antagonist, dose-dependently reduces neuropathic pain in the rat. J.Pharmacol.Exp.Ther. 2006 PMID: 16982702

Citations for A 740003 (13)

Showing 1 - 10 of 13 citations Showing All

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Citations are publications that use Bio-Techne products. Selected citations for A 740003 include:

De Marchi et al. (2019) The P2X₇ receptor modulates immune cells infiltration, ectonucleotidases expression and extracellular ATP levels in the tumor microenvironment. Oncogene. 2019;
PMID: 30655604
Zumerle et al. (2019) Intercellular Calcium Signaling Induced by ATP Potentiates Macrophage Phagocytosis. Cell Rep. 27:1
PMID: 30943393
Bergamin et al. (2019) Role of the P2X7 receptor in in vitro and in vivo glioma tumor growth. Oncotarget. 10:4840
PMID: 31448051
Gilbert et al. (2019) ATP in the tumour microenvironment drives expression of nfP2X7, a key mediator of cancer cell survival. Oncogene. 38:194
PMID: 30087439
Agrawal et al. (2016) P2X₇Rs are involved in cell death, growth and cellular signaling in primary human osteoblasts Bone. 95:91
PMID: 27856358
Englezou et al. (2015) P2X7R activation drives distinct IL-1 responses in dendritic cells compared to macrophages. Cytokine. 74:293
PMID: 26068648
Adamczyk et al. (2015) P2X7 receptor activation regulates rapid unconventional export of transglutaminase-2. J.Cell Sci.. 128:4615
PMID: 26542019
Song et al. (2015) Up-regulation of P2X7 receptors mediating proliferation of Schwann cells after sciatic nerve injury. J Cell Sci. 11:203
PMID: 25682129
Adamczyk et al. (2015) P2X7 receptor activation regulates rapid unconventional export of transglutaminase-2. Br J Pharmacol. 128:4615
PMID: 26542019
Ashpole et al. (2013) Loss of calcium/calmodulin-dependent protein kinase II activity in cortical astrocytes decreases glutamate uptake and induces neurotoxic release of ATP. J Biol Chem. 288:14599
PMID: 23543737
Hazleton et al. (2012) Purinergic receptors are required for HIV-1 infection of primary human macrophages. J Immunol. 188:4488
PMID: 22450808
Amoroso et al. (2012) The P2X7 receptor is a key modulator of aerobic glycolysis. Cell Death Dis. 3:e370
PMID: 22898868
Grol et al. (2012) P2X?-mediated calcium influx triggers a sustained, PI3K-dependent increase in metabolic acid production by osteoblast-like cells. Am J Physiol Endocrinol Metab. 302:E561
PMID: 22185840

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Showing 1 - 10 of 13 citations Showing All

Product Documents for A 740003

COA

Certificate of Analysis

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