Overview
Lyophilized Powder yes
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
- 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.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).
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
Lyophilized Powder
For research purposes only, not for human use
Last Update: 07/05/2024
Specifications
Citations
Citations
