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Description: Potent and selective P2X7 antagonist
Chemical Name: N-[1-[[(Cyanoamino)(5-quinolinylamino)methylene]amino]-2,2-dimethylpropyl]-3,4-dimethoxybenzeneacetamide
Purity: ≥97% (HPLC)
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 | ≥97% (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 Data for A 740003
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| 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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Product Datasheets for A 740003
References for A 740003
References are publications that support the biological activity of the product.
Honore et al (2006) 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. 319 1376 PMID: 16982702
King (2007) Novel P2X7 receptor antagonists ease the pain. Br.J.Pharmacol. 151 565 PMID: 17471176
Donnelly-Roberts et al (2009) Mammalian P2X7 receptor pharmacology: comparison of recombinant mouse, rat and human P2X7 receptors. Br.J.Pharmacol. 157 1203 PMID: 19558545
Amoroso et al (2015) The P2X7 receptor is a key modulator of the PI3K/GSK3β/VEGF signaling network: evidence in experimental neuroblastoma. Oncogene 34 5240 PMID: 25619831
If you know of a relevant reference for A 740003, please let us know.
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Keywords: A 740003, A 740003 supplier, A740003, potent, selective, P2X7, receptors, antagonists, purinergics, purinoceptors, P2X, Receptors, 3701, Tocris Bioscience
22 Citations for A 740003
Citations are publications that use Tocris products. Selected citations for A 740003 include:
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
De Marchi et al (2019) The P2X7 receptor modulates immune cells infiltration, ectonucleotidases expression and extracellular ATP levels in the tumor microenvironment. Oncogene PMID: 30655604
Bergamin et al (2019) Role of the P2X7 receptor in in vitro and in vivo glioma tumor growth. Oncotarget 10 4840 PMID: 31448051
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
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
Timothy S et al (2021) Differential Regulation of ATP- and UTP-Evoked Prostaglandin E2 and IL-6 Production from Human Airway Epithelial Cells. J Immunol 207 1275-1287 PMID: 34389624
Sung-Joong et al (2021) Roles of Cytokines in the Temporal Changes of Microglial Membrane Currents and Neuronal Excitability and Synaptic Efficacy in ATP-Induced Cortical Injury Model. Int J Mol Sci 22 PMID: 34202215
Colin W et al (2021) P2X4 Receptors Mediate Ca2+ Release from Lysosomes in Response to Stimulation of P2X7 and H1 Histamine Receptors. Int J Mol Sci 22 PMID: 34638832
Ketan et al (2021) Pannexin 1 Regulates Skeletal Muscle Regeneration by Promoting Bleb-Based Myoblast Migration and Fusion Through a Novel Lipid Based Signaling Mechanism. Front Cell Dev Biol 9 736813 PMID: 34676213
John P et al (2021) Src family kinases activity is required for transmitting purinergic P2X7 receptor signaling in cortical spreading depression and neuroinflammation. J Headache Pain 22 146 PMID: 34863113
Alberto et al (2017) P2X7 Receptor Induces Tumor Necrosis Factor-α Converting Enzyme Activation and Release to Boost TNF-α Production. Front Immunol 8 862 PMID: 28791020
Morley D et al (2022) Cathelicidins Induce Toll-Interacting Protein Synthesis to Prevent Apoptosis in Colonic Epithelium. J Innate Immun 1-18 PMID: 36116427
Zumerle et al (2019) Intercellular Calcium Signaling Induced by ATP Potentiates Macrophage Phagocytosis. Cell Rep 27 1 PMID: 30943393
Agrawal et al (2016) P2X7Rs are involved in cell death, growth and cellular signaling in primary human osteoblasts Bone 95 91 PMID: 27856358
Morley D et al (2020) Cathelicidin-mediated lipopolysaccharide signaling via intracellular TLR4 in colonic epithelial cells evokes CXCL8 production. Gut Microbes 12 1785802 PMID: 32658599
Carlos Amilcar et al (2020) Peripheral Inflammatory Hyperalgesia Depends on P2X7 Receptors in Satellite Glial Cells. Front Physiol 11 473 PMID: 32523543
Hazleton et al (2012) Purinergic receptors are required for HIV-1 infection of primary human macrophages. J Immunol 188 4488 PMID: 22450808
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
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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!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
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.