Home / P2X Receptor Antagonists / A 740003

A 740003

Catalog #: 3701
22 Citations Datasheet
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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: ≥97%

Product Details
Citations (22)
Supplemental Products
Reviews
Biological Activity Technical Data Background Product Datasheets Calculators

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

M.Wt:
474.55
Formula:
C26H30N6O3
Solubility:
Soluble to 20 mM in DMSO
Purity:
≥97%
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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. Intra-articular blockade of P2X7 receptor reduces the articular hyperalgesia and inflammation in the knee joint synovitis especially in female rats
    Cláudia Herrera Tambeli
    J Pain, 2016;0(0):.
  2. Accelerated tumor progression in mice lacking the ATP receptor P2X7.
    Adinolfi E, Capece M, Franceschini A, Falzoni S, Giuliani A, Rotondo A, Sarti A, Bonora M, Syberg S, Corigliano D, Pinton P, Jorgensen N, Abelli L, Emionite L, Raffaghello L, Pistoia V, Di Virgilio F
    Cancer Res, 2015;75(4):635-44.
  3. Purinergic receptors are required for HIV-1 infection of primary human macrophages.
    Hazleton JE, Berman JW, Eugenin EA
    J. Immunol., 2012;188(9):4488-95.
  4. Sphingosine regulates the NLRP3-inflammasome and IL-1beta release from macrophages.
    Luheshi NM, Giles JA, Lopez-Castejon G, Brough D
    Eur. J. Immunol., 2011;42(3):716-25.
  5. Systemic blockade of P2X7 receptor protects against sepsis-induced intestinal barrier disruption
    X Wu, J Ren, G Chen, L Wu, X Song, G Li, Y Deng, G Wang, G Gu, J Li
    Sci Rep, 2017;7(1):4364.
  6. P2X7 receptor antagonism modulates IL-1? and MMP9 in human atherosclerotic vessels
    M Lombardi, ME Mantione, D Baccellier, D Ferrara, R Castellano, R Chiesa, O Alfieri, C Foglieni
    Sci Rep, 2017;7(1):4872.
  7. The P2X7 Receptor Primes IL-1? and the NLRP3 Inflammasome in Astrocytes Exposed to Mechanical Strain
    F Albalawi, W Lu, JM Beckel, JC Lim, SA McCaughey, CH Mitchell
    Front Cell Neurosci, 2017;11(0):227.
  8. 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
  9. Novel P2X7 receptor antagonists ease the pain.
    King
    Br.J.Pharmacol., 2007;151:565
  10. Mammalian P2X7 receptor pharmacology: comparison of recombinant mouse, rat and human P2X7 receptors.
    Donnelly-Roberts et al.
    Br.J.Pharmacol., 2009;157:1203
  11. The P2X7 receptor is a key modulator of the PI3K/GSK3β/VEGF signaling network: evidence in experimental neuroblastoma.
    Amoroso et al.
    Oncogene, 2015;34:5240

Product Datasheets

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Citations for A 740003

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

22 Citations: Showing 1 - 10

  1. Cathelicidins Induce Toll-Interacting Protein Synthesis to Prevent Apoptosis in Colonic Epithelium.
    Authors: Morley D Et al.
    J Innate Immun  2022;:1-18
  2. Pannexin 1 Regulates Skeletal Muscle Regeneration by Promoting Bleb-Based Myoblast Migration and Fusion Through a Novel Lipid Based Signaling Mechanism.
    Authors: Ketan Et al.
    Front Cell Dev Biol  2021;9:736813
  3. Src family kinases activity is required for transmitting purinergic P2X7 receptor signaling in cortical spreading depression and neuroinflammation.
    Authors: John P Et al.
    J Headache Pain  2021;22:146
  4. P2X4 Receptors Mediate Ca2+ Release from Lysosomes in Response to Stimulation of P2X7 and H1 Histamine Receptors.
    Authors: Colin W Et al.
    Int J Mol Sci  2021;22
  5. Roles of Cytokines in the Temporal Changes of Microglial Membrane Currents and Neuronal Excitability and Synaptic Efficacy in ATP-Induced Cortical Injury Model.
    Authors: Sung-Joong Et al.
    Int J Mol Sci  2021;22
  6. Differential Regulation of ATP- and UTP-Evoked Prostaglandin E2 and IL-6 Production from Human Airway Epithelial Cells.
    Authors: Timothy S Et al.
    J Immunol  2021;207:1275-1287
  7. Cathelicidin-mediated lipopolysaccharide signaling via intracellular TLR4 in colonic epithelial cells evokes CXCL8 production.
    Authors: Morley D Et al.
    Gut Microbes  2020;12:1785802
  8. Peripheral Inflammatory Hyperalgesia Depends on P2X7 Receptors in Satellite Glial Cells.
    Authors: Carlos Amilcar Et al.
    Front Physiol  2020;11:473
  9. ATP in the tumour microenvironment drives expression of nfP2X7, a key mediator of cancer cell survival.
    Authors: Gilbert Et al.
    Oncogene  2019;38:194
  10. Intercellular Calcium Signaling Induced by ATP Potentiates Macrophage Phagocytosis.
    Authors: Zumerle Et al.
    Cell Rep  2019;27:1
  11. Role of the P2X7 receptor in in vitro and in vivo glioma tumor growth.
    Authors: Bergamin Et al.
    Oncotarget  2019;10:4840
  12. The P2X7 receptor modulates immune cells infiltration, ectonucleotidases expression and extracellular ATP levels in the tumor microenvironment.
    Authors: De Marchi Et al.
    Oncogene  2019;
  13. P2X7 Receptor Induces Tumor Necrosis Factor-α Converting Enzyme Activation and Release to Boost TNF-α Production.
    Authors: Alberto Et al.
    Front Immunol  2017;8:862
  14. P2X7Rs are involved in cell death, growth and cellular signaling in primary human osteoblasts
    Authors: Agrawal Et al.
    Bone  2016;95:91
  15. P2X7R activation drives distinct IL-1 responses in dendritic cells compared to macrophages.
    Authors: Englezou Et al.
    Cytokine  2015;74:293
  16. P2X7 receptor activation regulates rapid unconventional export of transglutaminase-2.
    Authors: Adamczyk Et al.
    Br J Pharmacol  2015;128:4615
  17. P2X7 receptor activation regulates rapid unconventional export of transglutaminase-2.
    Authors: Adamczyk Et al.
    J.Cell Sci.  2015;128:4615
  18. Up-regulation of P2X7 receptors mediating proliferation of Schwann cells after sciatic nerve injury.
    Authors: Song Et al.
    J Cell Sci  2015;11:203
  19. 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
  20. The P2X7 receptor is a key modulator of aerobic glycolysis.
    Authors: Amoroso Et al.
    Cell Death Dis  2012;3:e370
  21. P2X?-mediated calcium influx triggers a sustained, PI3K-dependent increase in metabolic acid production by osteoblast-like cells.
    Authors: Grol Et al.
    Am J Physiol Endocrinol Metab  2012;302:E561
  22. Purinergic receptors are required for HIV-1 infection of primary human macrophages.
    Authors: Hazleton Et al.
    J Immunol  2012;188:4488

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