UK-78282 hydrochloride

A Blocker of KV1.3 and KV1.4 K+ Channels
    Cat #: U-100
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 466.1
    Purity: >95%
    Effective concentration 200 nM - 200 µM.
      • UK-78282 hydrochloride
    Chemical name 4-(benzhydryloxymethyl)-1-[3-(4-methoxyphenyl)propyl]piperidine;hydrochloride.
    Molecular formula C29H36ClNO2.
    CAS No.: 136647-02-4.
    Activity UK-78282 hydrochloride blocks KV1.3 and KV1.4 in T lymphocytes1.
      • 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 200 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.
      • UK-78282 hydrochloride
        Alomone Labs UK-78282 hydrochloride blocks KV1.3 channels heterologously expressed in Xenopus oocytes.
        A. Time course of 200 μM UK-78282 hydrochloride (#U-100) reversible inhibitory action on KV1.3 current amplitude. Ramp stimulation; 100 ms from holding potential -100 mV to +50 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. Hanson, D.C. et al. (1999) Br. J. Pharmacol. 126, 1707.
      • UK-78282 hydrochloride is a novel piperidine blocker of the T lymphocyte voltage-gated K+ channel, KV1.3 and KV1.4 with IC50 values of 0.28 and 0.17 μM respectively. UK-78282 suppresses T lymphocyte mitogenesis and leads to membrane depolarization. UK-78282 also blocks KV1.4 expressed in heart and brain. UK-78282 preferentially blocks the C-type inactivated state of the KV1.3 channel. KV1.3 mutants containing hydrophobic residues that might prefer to be buried, transition slowly into the C-type inactivated conformation and are insensitive to block by UK-78282, possibly because of the inability of the drug to bind the channel. UK-78282 hydrochloride serves as an experimental tool to probe the conformational changes in KV1.3 leading to C-type inactivation and to further define the critical physiological role of KV1.3 in T lymphocyte activation1.
    Target KV1.3, KV1.4 K+ channels
    Last update: 13/11/2019

    UK-78282 hydrochloride (#U-100) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use