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CP 465022 hydrochloride

A Selective, Non-Competitive Antagonist of AMPA Receptor and a Modulator of NaV1.6 Channels
Cat #: C-335
  • Lyophilized Powder
  • Bioassay Tested
    • Source Synthetic
    MW: 499.4
    Purity: >97% (HPLC)
    Effective concentration 25 nM - 25 µM.
    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.
    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.

      • Lazaro, J.T. et al. (2002) Neuropharmacology 42, 143.

      • 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.
      • 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.
      • Zhang, W. et al. (2006) Biophys. J. 91, 1336.
      • Lazaro, J.T. et al. (2002) Neuropharmacology 42, 143.
      • CP 465022 hydrochloride is a selective, noncompetitive 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. In human neuronal hNT cell line an IC50 of 15 nM can be observed. The inhibitory effect of CP develops slowly and inhibition is also slow to reverse upon compound washout suggesting a slow rate of interaction between CP and the AMPA receptor. In addition, this is explained by CP’s high lypophilicity and protein binding. CP reduces the efficacy of kainate to activate AMPA receptors at any kainate concentration indicating it binds to a site different from the agonist site. Inhibition of the AMPA receptor by CP is neither use-dependent nor voltage dependent1. CP significantly inhibits the persistent inward Na+ current of the NaV1.6 channel in a dose dependent manner. This requires caution when ascribing actions to the AMPA receptor based on CP.
    Target AMPA receptors, NaV1.6 Na+ channels
    Lyophilized Powder
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    Last update: 10/03/2019

    CP 465022 hydrochloride (#C-335) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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