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A-740003

N-(1-{[(Cyanoimino)(5-quinolinylamino)methyl]amino}-2,2-dimethylpropyl)-2-(3,4-dimethoxyphenyl)acetamide

A Potent and Selective Antagonist of P2X7 Receptors

Cat #: A-420
Alternative Name N-(1-{[(Cyanoimino)(5-quinolinylamino)methyl]amino}-2,2-dimethylpropyl)-2-(3,4-dimethoxyphenyl)acetamide
Lyophilized Powder yes
  • Bioassay Tested
    • Source Synthetic
    MW: 474.55
    Purity: >96% (HPLC)
    Effective concentration 10 nM – 1 µM.
    Structure
    Chemical name N-[1-[(E)-[(cyanoamino)-(quinolin-5-ylamino)methylidene]amino]-2,2-dimethylpropyl]-2-(3,4-dimethoxyphenyl)acetamide.
    Molecular formula C26H30N6O3.
    CAS No.: 861393-28-4
    PubChem CID 11351968
    Activity A-740003 is a potent and selective competitive antagonist of P2X7 receptors with IC50 values of 18 nM, 44 nM and 0.68 µM for rat, human and mouse receptors, respectively. A-740003 reduces neuropathic pain and tumor growth in vivo1,2.
    References-Activity
    1. Honore, P. et al. (2006) J. Pharmacol. Exp. Ther. 319, 1376.
    2. Donnelly-Roberts, D.L. et al. (2009) Br. J. Pharmacol. 157, 1203.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Solubility Soluble in DMSO. Centrifuge all products before handling (10000 x g 5 min).
    Storage of solutions -20°C. It is recommended to aliquot stock solutions to prevent repeated thawing and freezing.
    Our bioassay
    • Alomone Labs A-740003 inhibits human P2X7 receptors expressed in HEK-293 cells.
      Alomone Labs A-740003 inhibits human P2X7 receptors expressed in HEK-293 cells.
      Dose-response curve of hP2X7 inhibition by A-740003 (#A-420). Cells were loaded with Fluo-8 NW dye, incubated with increasing concentrations of A-740003, and stimulated with 80 µM BzATP. Changes in intracellular Ca2+ following agonist application were detected as changes in maximum relative fluorescence (RLU) using FLIPRTETRA™. IC50 was calculated at 72 nM.
    References - Scientific background
    1. Honore, P. et al. (2006) J. Pharmacol. Exp. Ther. 319, 1376.
    2. Donnelly-Roberts, D.L. et al. (2009) Br. J. Pharmacol. 157, 1203.
    Scientific background

    A-740003 is a potent, selective, and competitive antagonist of the P2X7 receptor, with IC50 values of 18 nM and 44 nM for rat and human P2RX7, respectively1. The compound shows weak or no activity on other P2 receptors.

    A-740003 has the ability to reduce neuropathic pain and tumor growth in vivo. Systemic administration of A-740003 in rat produces dose-dependent antinociception in a spinal nerve ligation model1,2.

    The P2X receptor family includes seven receptor subtypes: P2X1–P2X7. P2X7 receptors participate in a variety of cellular responses such as membrane permeabilization, activation of caspases, cytokine release, cell proliferation, and apoptosis. They are highly expressed on immune cells including glial cells, macrophages and other antigen-presenting cells1,2.

    Target P2X7 receptors
    Lyophilized Powder
    Last update: 11/04/2021

    A-740003 (#A-420) is a highly pure, synthetic, and biologically active compound.

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    For research purposes only, not for human use
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