Free shipping starts now, no minimum, no coupons required!

UK-78282 hydrochloride

A Blocker of KV1.3 and KV1.4 K+ Channels
Cat #: U-100
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 466.1
    Purity: >95%
    Effective concentration 200 nM - 200 µM.
    Structure
    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.
    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 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.
    Our bioassay
    • Alomone Labs UK-78282 hydrochloride blocks KV1.3 channels heterologously expressed in Xenopus oocytes.
      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.
    Scientific background 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: 23/08/2020

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

    For research purposes only, not for human use
    Shipping and Ordering information

    Resources