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AACBA hydrochloride

N-(Adamantan-1-ylmethyl)-5-[(3R-aminopyrrolidin-1-yl)methyl]-2-chloro-benzamide hydrochloride, GSK314181A

A Potent and Selective Antagonist of P2X7 Receptors

Cat #: A-410
Alternative Name N-(Adamantan-1-ylmethyl)-5-[(3R-aminopyrrolidin-1-yl)methyl]-2-chloro-benzamide hydrochloride, GSK314181A
Lyophilized Powder yes
  • Bioassay Tested
    • Source Synthetic
    MW: 438.43
    Purity: >99%
    Effective concentration 1-100 nM.
    Structure
    Chemical name N-(Adamantan-1-ylmethyl)-5-[(3R-aminopyrrolidin-1-yl)methyl]-2-chloro-benzamide hydrochloride.
    Molecular formula C23H33Cl2N3O (C23H32ClN3O · HCl).
    Activity AACBA hydrochloride is a potent and selective antagonist of P2X7 receptors, shown to inhibit human and rat P2X7 receptors with IC50 values of 18 nM and 29 nM, respectively. Active in vivo on acute models of pain and inflammation1.
    References-Activity
    1. Broom, D.C. et al. (2008) J. Pharmacol. Exp. Ther. 327, 620.
    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 200 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 AACBA hydrochloride inhibits human P2X7 receptors expressed in HEK-293 cells.
      Alomone Labs AACBA hydrochloride inhibits human P2X7 receptors expressed in HEK-293 cells.
      Dose-response curve of hP2X7 inhibition by AACBA hydrochloride (#A-410). Cells were loaded with Fluo-8 NW dye, incubated with increasing concentrations of AACBA 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 19.3 nM.
    References - Scientific background
    1. Broom, D.C. et al. (2008) J. Pharmacol. Exp. Ther. 327, 620.
    2. Pijacka, W. et al. (2016) Nat. Med. 10, 1151.
    Scientific background

    AACBA hydrochloride is a potent and selective antagonist of P2X7 receptors. It inhibits human and rat P2X7 receptors with IC50 values of 18 nM and 29 nM, respectively1.

    AACBA reduces interleukin-6 release in a dose-dependent manner and prevents or reverses carrageenan-induced paw edema and mechanical hypersensitivity in acute in vivo models of pain and inflammation1.

    P2X receptors are a family of ion channels gated by ATP, a ubiquitous energy donor and receptor ligand in living cells. P2X receptors are widely expressed in neuronal, muscular, epithelial and immune cells and play a pivotal role in models of various pain conditions. P2X7 receptor mediates the release of proinflammatory cytokines known to have roles in inflammatory/immune conditions and pain1,2.

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

    AACBA hydrochloride (#A-410) 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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