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CAY10593 (VU0155069)

(S)-N-(1-(4-(5-Chloro-2-oxo-2,3-dihydro-1H-benzo[d]imidazol-1-yl)piperidin-1-yl)propan-2-yl)-2-naphthamide.

An Antagonist of P2X7 Receptors and an Inhibitor of Phospholipase D1

Cat #: C-385
Alternative Name (S)-N-(1-(4-(5-Chloro-2-oxo-2,3-dihydro-1H-benzo[d]imidazol-1-yl)piperidin-1-yl)propan-2-yl)-2-naphthamide.
Lyophilized Powder yes
  • Bioassay Tested
    • Source Synthetic
    MW: 462.98
    Purity: >95%
    Effective concentration 1-10 µM.
    Structure
    Chemical name N-[(2S)-1-[4-(5-chloro-2-oxo-3H-benzimidazol-1-yl)piperidin-1-yl]propan-2-yl]naphthalene-2-carboxamide.
    Molecular formula C26H27ClN4O2.
    CAS No.: 1130067-06-9
    PubChem CID 53393949
    Activity CAY10593 (VU0155069) is an antagonist of purinergic P2X7 receptors, shown to inhibit ATP-induced ethidium+ uptake in RPMI 8226 cells with IC50 of 2 µM1. It is also a potent and selective inhibitor of phospholipase D1 (IC50 of 46 and 933 nM for PLD1 and PLD2, respectively)2.
    References-Activity
    1. Pupovac, A. et al. (2013) Purinergic Signal. 9, 609.
    2. Lewis, J.A. et al. (2009) Bioorg. Med. Chem. Lett. 19, 1916.
    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 CAY10593 (VU0155069) inhibits human P2X7 receptors expressed in HEK-293 cells.
      Alomone Labs CAY10593 (VU0155069) inhibits human P2X7 receptors expressed in HEK-293 cells.
      Dose-response curve of hP2X7 inhibition by CAY10593 (VU0155069) (#C-385). Cells were loaded with Fluo-8 NW dye, incubated with increasing concentrations of CAY10593, and stimulated by 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 5.9 µM.
    References - Scientific background
    1. Pupovac, A. et al. (2013) Purinergic Signal. 9, 609.
    2. Lewis, J.A. et al. (2009) Bioorg. Med. Chem. Lett. 19, 1916.
    Scientific background

    CAY10593 (VU0155069) is an antagonist of purinergic P2X7 receptors and an inhibitor of phospholipase D1 (PLD1)1. CAY10593 inhibits ATP-induced ethidium+ uptake in RPMI 8226 cells expressing P2X7 receptors in a concentration-dependent manner with an IC50 value of 2 µM1.

    The P2X receptors are a family of ligand-gated ion channels present on various cell types. P2X receptors are activated by extracellular ATP and play an important role in many disease states, including inflammatory, immune, neoplastic, musculoskeletal, and neurological disorders1,2.

    Target P2X7 receptors, Phospholipase D1 (PLD1)
    Lyophilized Powder
    Last update: 06/11/2022

    CAY10593 (VU0155069) (#C-385) 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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