A 740003

Catalog # Availability Size / Price Qty
A 740003 | CAS No. 861393-28-4 | P2X Receptor Antagonists
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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: ≥98%

Product Details
Citations (13)
Supplemental Products

Biological Activity

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.

Technical Data

Soluble to 20 mM in DMSO
Store at +4°C

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.

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Citations for A 740003

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

13 Citations: Showing 1 - 10

  1. ATP in the tumour microenvironment drives expression of nfP2X7, a key mediator of cancer cell survival.
    Authors: Gilbert Et al.
    Oncogene  2019;38:194
  2. Intercellular Calcium Signaling Induced by ATP Potentiates Macrophage Phagocytosis.
    Authors: Zumerle Et al.
    Cell Rep  2019;27:1
  3. Role of the P2X7 receptor in in vitro and in vivo glioma tumor growth.
    Authors: Bergamin Et al.
    Oncotarget  2019;10:4840
  4. The P2X7 receptor modulates immune cells infiltration, ectonucleotidases expression and extracellular ATP levels in the tumor microenvironment.
    Authors: De Marchi Et al.
    Oncogene  2019;
  5. P2X7Rs are involved in cell death, growth and cellular signaling in primary human osteoblasts
    Authors: Agrawal Et al.
    Bone  2016;95:91
  6. P2X7R activation drives distinct IL-1 responses in dendritic cells compared to macrophages.
    Authors: Englezou Et al.
    Cytokine  2015;74:293
  7. P2X7 receptor activation regulates rapid unconventional export of transglutaminase-2.
    Authors: Adamczyk Et al.
    J.Cell Sci.  2015;128:4615
  8. P2X7 receptor activation regulates rapid unconventional export of transglutaminase-2.
    Authors: Adamczyk Et al.
    Br J Pharmacol  2015;128:4615
  9. Up-regulation of P2X7 receptors mediating proliferation of Schwann cells after sciatic nerve injury.
    Authors: Song Et al.
    J Cell Sci  2015;11:203
  10. 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


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