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AZD-9056 hydrochloride

N-(1-Adamantylmethyl)-2-chloro-5-[3-(3-hydroxypropylamino)propyl]benzamide hydrochloride

A Potent and Selective Antagonist of P2X7 Receptors

Cat #: A-425
Alternative Name N-(1-Adamantylmethyl)-2-chloro-5-[3-(3-hydroxypropylamino)propyl]benzamide hydrochloride
Lyophilized Powder yes
  • Bioassay Tested
    • Source Synthetic
    MW: 455.46
    Purity: >97%
    Effective concentration 1-100 nM.
    Structure
    Chemical name N-(1-adamantylmethyl)-2-chloro-5-[3-(3-hydroxypropylamino)propyl]benzamide hydrochloride.
    Molecular formula C24H36Cl2N2O2 (C24H35ClN2O2 · HCl).
    CAS No.: 345303-91-5
    PubChem CID 10161380
    Activity AZD-9056 is a potent and selective, orally bioavailable antagonist of the purinergic P2X7 receptor, shown to inhibit YoPro1 uptake in HEK–hP2X7 cells with IC50 of 11.2 nM1. AZD-9056 shows pain-relieving and anti-inflammatory effects in vivo2.
    References-Activity
    1. Seeland, S. et al. (2015) Pharmacol. Res. Perspect. 3, e00123.
    2. Hu, H. et al. (2016) Int. J. Mol. Med. 38, 1922.
    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 AZD-9056 hydrochloride inhibits human P2X7 receptors expressed in HEK-293 cells.
      Alomone Labs AZD-9056 hydrochloride inhibits human P2X7 receptors expressed in HEK-293 cells.
      Dose-response curve of hP2X7 inhibition by AZD-9056 hydrochloride (#A-425). Cells were loaded with Fluo-8 NW dye, incubated with increasing concentrations of AZD-9056 hydrochloride, 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 12 nM.
    References - Scientific background
    1. Seeland, S. et al. (2015) Pharmacol. Res. Perspect. 3, e00123.
    2. Hu, H. et al. (2016) Int. J. Mol. Med. 38, 1922.
    3. Stokes, L. et al. (2006) Br. J. Pharmacol. 149, 880.
    4. Donnelly-Roberts, D.L. et al. (2009) Br. J. Pharmacol. 157, 1203
    Scientific background

    AZD-9056 hydrochloride is an adamantane amide that acts as a potent and selective antagonist of P2X7 receptors. It inhibits YoPro1 (membrane-impermeable fluorescent dye) uptake in HEK–hP2X7 cells with IC50 value of 11.2 nM1. Studies show that treatment with AZD-9056 exerts pain-relieving and anti-inflammatory effects1,2.

    The P2X7 receptor is a member of the ligand-gated ion channels activated by extracellular ATP. There are 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. P2X7 receptors are highly expressed throughout autonomic, sensory and central neurons and in visceral smooth muscle, immune cells and epithelia3,4.

    Target P2X7 receptors
    Lyophilized Powder
    Last update: 06/11/2022

    AZD-9056 hydrochloride (#A-425) 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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