Catalog Number: 3701
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.
Background References
  1. 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.
    Honore et al.
    J.Pharmacol.Exp.Ther., 2006;319:1376
  2. Novel P2X7 receptor antagonists ease the pain.
    King
    Br.J.Pharmacol., 2007;151:565
  3. Mammalian P2X7 receptor pharmacology: comparison of recombinant mouse, rat and human P2X7 receptors.
    Donnelly-Roberts et al.
    Br.J.Pharmacol., 2009;157:1203
  4. The P2X7 receptor is a key modulator of the PI3K/GSK3β/VEGF signaling network: evidence in experimental neuroblastoma.
    Amoroso et al.
    Oncogene, 2015;
Citations:

The citations listed below are publications that use Tocris products. Selected citations for A 740003 include:

7 Citations: Showing 1 - 7
Filter your results:

  1. P2X7Rs are involved in cell death, growth and cellular signaling in primary human osteoblasts
    Authors: Agrawal Et al.
    Bone 2016;95:91
  2. P2X7R activation drives distinct IL-1 responses in dendritic cells compared to macrophages.
    Authors: Englezou Et al.
    Cytokine 2015;74:293
  3. P2X7 receptor activation regulates rapid unconventional export of transglutaminase-2.
    Authors: Adamczyk Et al.
    J.Cell Sci. 2015;128:4615
  4. P2X7 receptor activation regulates rapid unconventional export of transglutaminase-2.
    Authors: Adamczyk Et al.
    Br J Pharmacol 2015;128:4615
  5. Up-regulation of P2X7 receptors mediating proliferation of Schwann cells after sciatic nerve injury.
    Authors: Song Et al.
    J Cell Sci 2015;11:203
  6. Loss of calcium/calmodulin-dependent protein kinase II activity in cortical astrocytes decreases glutamate uptake and induces neurotoxic release of ATP.
    Authors: Ashpole Et al.
    J Biol Chem 2013;288:14599
  7. Purinergic receptors are required for HIV-1 infection of primary human macrophages.
    Authors: Hazleton Et al.
    J Immunol 2012;188:4488

Have you used A 740003?

Submit a review and receive a $25US/€18/£15/$25CAN amazon gift card if you include an image - $10US/€7/£6/$10CAN Amazon card for reviews without an image. Limited to verified customers in USA, Canada and Europe.

Tocris Bioscience is the leading supplier of novel and exclusive tools for life science research with over 30 years' experience in the industry. Tocris is a Bio-Techne brand.

Order Details

Note:

Contact Information

Calculators

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

R&D Systems Guarantee

or select another batch: 

Feedback

Customer Information