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CP 339818 hydrochloride

A Blocker of KV1.3 and KV1.4 K+ Channels

Cat #: C-115
Lyophilized Powder yes
  • Bioassay Tested
    • Source Synthetic
    MW: 340.9
    Purity: >98%
    Effective concentration 1-200 µM.
    Structure
    Chemical name N-[1-(Phenylmethyl)-4(1H)-quinolinylidene]-1 pentanamine hydrochloride.
    Molecular formula C21H25ClN2.
    CAS No.: 185855-91-8
    Activity CP 339818 hydrochloride is a KV1.3 and KV1.4 channel blocker1.
    References-Activity
    1. Hanson, D.C. et al. (1999) Br. J. Pharmacol. 126, 1707.
    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 20 mM in DMSO. Centrifuge all product preparations before use (10000 x g for 1 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
    Our bioassay
    • Alomone Labs CP 339818 hydrochloride inhibits KV1.3 channels heterologously expressed in Xenopus oocytes.
      Alomone Labs CP 339818 hydrochloride inhibits KV1.3 channels heterologously expressed in Xenopus oocytes.
      A. Time course of reversible current inhibition of KV1.3 current amplitude by 200 μM CP 339818 hydrochloride (#C-115). Ramp stimulation; 100 ms from holding potential -100 mV to +20 mV, delivered every 10 seconds. B. Superimposed current traces of control and inhibited current as indicated (taken from the experiment in A).
    References - Scientific background
    1. Nguyen, A. et al. (1996) Mol. Pharmacol. 50, 1672.
    Scientific background CP 339818 hydrochloride is a potent KV1.3 channel antagonist that preferentially binds to the C-type inactivated state of the channel. It appears to recognize only the inactivated conformation of KV1.3. CP 339818 hydrochloride inhibits KV1.3 expressed in the brain and in T lymphocyte cells with an IC50 value of ~200 nM. In addition to its effect on KV1.3, CP 339818 inhibits the Shaker-related A-type K+ channel, KV1.4, expressed in brain cells with an IC50 of ~300 nM. CP 339818 is a significantly less potent blocker at KV1.1, KV1.2, KV1.5, KV1.6, KV3.1-4, and KV4.2. CP 339818 is valuable for immune system studies, where the absence of KV1.4 makes it functionally selective for KV1.3, and it has shown suppression of T cell activation. CP 339818 hydrochloride is also valuable for the study of KV1.4 function1.
    Target KV1.3, KV1.4 K+ channels
    Lyophilized Powder
    Last update: 12/08/2021

    CP 339818 hydrochloride (#C-115) 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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