A 740003

Cat. No. 3701

A 740003 C26H30N6O3 [861393-28-4]

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Chemical Name: N-[1-[[(Cyanoamino)(5-quinolinylamino)methylene]amino]-2,2-dimethylpropyl]-3,4-dimethoxybenzeneacetamide

Biological Activity

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.

Technical Data

M.Wt:
474.55
Formula:
C26H30N6O3
Solubility:
Soluble to 20 mM in DMSO
Purity:
>98 %
Storage:
Store at +4°C
CAS No:
861393-28-4

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 / Product Datasheet / Safety Data Sheet

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.

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.

King (2007) Novel P2X7 receptor antagonists ease the pain. Br.J.Pharmacol. 151 565. PMID: 17471176.

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.

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Citations are publications that use Tocris products. Selected citations for A 740003 include:

Adamczyk et al (2015) P2X7 receptor activation regulates rapid unconventional export of transglutaminase-2. J.Cell Sci. 128 4615. PMID: 26542019.

Adamczyk et al (2015) P2X7 receptor activation regulates rapid unconventional export of transglutaminase-2. Br J Pharmacol 128 4615. PMID: 26542019.

Englezou et al (2015) P2X7R activation drives distinct IL-1 responses in dendritic cells compared to macrophages. Cytokine 74 293. PMID: 26068648.

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.

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.

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Keywords: A 740003, supplier, A740003, potent, selective, P2X7, receptors, antagonists, purinergics, purinoceptors, Tocris Bioscience, Purinergic (P2X) Receptor Antagonist products

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