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CP 465022 hydrochloride

A Selective, Non-Competitive Antagonist of AMPA Receptors and a Modulator of NaV1.6 Channels

Cat #: C-335
Lyophilized Powder yes
  • Bioassay Tested
    • Source Synthetic
    MW: 499.4
    Purity: >97% (HPLC)
    Effective concentration 25 nM - 25 µM.
    Structure
    Chemical name 3-(2-chlorophenyl)-2-[(E)-2-[6-(diethylaminomethyl)pyridin-2-yl]ethenyl]-6-fluoroquinazolin-4-one;hydrochloride.
    Molecular formula C26H25Cl2FN4O.
    CAS No.: 199655-36-2
    PubChem CID 53251536
    Activity CP 465022 is a selective, non-competitive AMPA receptor antagonist. It inhibits AMPA receptor-mediated currents in rat cortical neurons (IC50 25 nM)1. It also partially blocks the persistent components of NaV1.6 channel activity2.
    References-Activity
    1. Lazaro, J.T. et al. (2002) Neuropharmacology 42, 143.
    2. Welch, N.C. et al. (2008) Neuropharmacology 55, 1165.
    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 >25 mM in DMSO. Centrifuge all product preparations before use.
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
    Our bioassay
    • Alomone Labs CP 465022 hydrochloride inhibits GluA1 channels expressed in Xenopus oocytes.
      Alomone Labs CP 465022 hydrochloride inhibits GluA1 channels expressed in Xenopus oocytes.
      A. Time course of reversible inhibition by 5 μM and 25 μM CP 465022 hydrochloride (#C-335) of glutamate-activated current (100 μM, every 100 s, at holding potential -80 mV). B. Superimposed current traces of control and inhibited currents (as indicated), taken from A.
    References - Scientific background
    1. Zhang, W. et al. (2006) Biophys. J. 91, 1336.
    2. Lazaro, J.T. et al. (2002) Neuropharmacology 42, 143.
    3. Welch, N.C. et al. (2008) Neuropharmacology 55, 1165.
    Scientific background

    CP 465022 hydrochloride is a selective, non-competitive antagonist of the AMPA receptor and a modulator of the voltage-gated sodium NaV1.6 channel. It has an IC50 value of 25 nM for AMPA mediated currents in rat cortical neurons and in human neuronal hNT cell lines, an IC50 of 15 nM can be observed. The inhibitory effect of CP develops slowly. The reversal of its inhibition is also slow upon compound washout, suggesting a slow rate of interaction between CP and the AMPA receptor. This may also be attributed to CP’s high lypophilicity and protein binding. CP reduces the efficacy of kainate activation of AMPA receptors at any kainate concentration, indicating that it binds to a site other than the agonist site. Inhibition of the AMPA receptor by CP is neither use-dependent nor voltage-dependent1,2. CP significantly inhibits the persistent inward Na+ current of the NaV1.6 channel in a dose-dependent manner3. This requires caution when ascribing actions to the AMPA receptor based on CP.

    Target AMPA receptors, NaV1.6 Na+ channels
    Lyophilized Powder
    Last update: 02/01/2022

    CP 465022 hydrochloride (#C-335) 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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