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AZ 10606120 dihydrochloride

N-[2-[[2-[(2-Hydroxyethyl)amino]ethyl]amino]-5-quinolinyl]- 2-tricyclo[3.3.1.13,7]dec-1-ylacetamide dihydrochloride

A Potent and Selective Antagonist of P2X7 Receptors

Cat #: A-405
Alternative Name N-[2-[[2-[(2-Hydroxyethyl)amino]ethyl]amino]-5-quinolinyl]- 2-tricyclo[3.3.1.13,7]dec-1-ylacetamide dihydrochloride
Lyophilized Powder yes
  • Bioassay Tested
    • Source Synthetic
    MW: 495.49
    Purity: >97%
    Effective concentration 1-100 nM.
    Structure
    Chemical name 2-(1-adamantyl)-N-[2-[2-(2-hydroxyethylamino)ethylamino]quinolin-5-yl]acetamide;dihydrochloride.
    Molecular formula C25H36Cl2N4O2 (C25H34N4O2 · 2HCl).
    CAS No.: 607378-18-7
    PubChem CID 56972227
    Activity AZ 10606120 dihydrochloride is a potent and selective non-competitive antagonist of P2X7 receptors, acting as a negative allosteric modulator shown to inhibit human P2X7 receptors with pIC50 of 8.1-8.91-3. It also inhibits growth and neoangiogenesis of P2X7-expressing tumors in mice4.
    References-Activity
    1. Michel, A.D. et al. (2008) Br. J. Pharmacol. 153, 737.
    2. Bhattacharya, A. et al. (2013) Br. J. Pharmacol. 170, 624.
    3. Allsopp, R.C. et al. (2017) Sci. Rep. 7, 725.
    4. Adinolfi, E. et al. (2012) Cancer Res. 72, 2957.
    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 up to 100 mM in DMSO and up to 20 mM in water. Centrifuge all products before handling (10000 x g 5 min).
    Storage of solutions Store at -20°C. It is recommended to aliquot stock solutions to prevent repeated thawing and freezing.
    Our bioassay
    • Alomone Labs AZ 10606120 dihydrochloride inhibits human P2X7 receptors expressed in HEK-293 cells.
      Alomone Labs AZ 10606120 dihydrochloride inhibits human P2X7 receptors expressed in HEK-293 cells.
      Dose-response curve of hP2X7 inhibition by AZ 10606120 dihydrochloride (#A-405). Cells were loaded with Fluo-8 NW dye, incubated with increasing concentrations of AZ 10606120 dihydrochloride, 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 8.15 nM.
    References - Scientific background
    1. Michel, A.D. et al. (2008) Br. J. Pharmacol. 153, 737.
    2. Allsopp, R.C. et al. (2017) Sci. Rep. 7, 725.
    Scientific background

    AZ 10606120 dihydrochloride is a potent and selective noncompetitive antagonist of the P2X7 receptor with IC50 value of ~10 nM2. The compound shows little or no effect at other P2X receptor subtypes1,2. In studies conducted in animal models, AZ 10606120 treatment shows antidepressant effects and reduces tumor growth2.

    P2X receptors are a family of ligand-gated cation channels activated by the binding of extracellular ATP. Seven members of this family have been identified and function in homomeric or heteromeric combinations. P2X7 receptor is a therapeutic target due to its potential involvement in pain and inflammatory disorders1,2.

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

    AZ 10606120 dihydrochloride (#A-405) 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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