ICA-27243

A Potent and Selective Opener of KCNQ2 and KCNQ3 K+ Channels
Cat #: I-130
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 268.64
    Purity: >99%
    Effective concentration 0.5-50 µM.
    Structure
    Chemical name N-(6-Chloro-pyridin-3-yl)-3,4-difluoro-benzamide.
    Molecular formula C12H7ClF2N2O.
    CAS No.: 325457-89-4.
    Activity ICA-27243 is a potent and selective KCNQ channel modulator (enhancer)1 with EC50 ~ 1 µM.
    References - Activity
    1. Padilla, K. et al. (2009) Neurosci. Lett. 465, 138.

    Storage before reconstitution 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.
    Reconstitution 100 mM DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage after reconstitution Up to four weeks at 4°C or three months at -20°C.
    Our bioassay
    Alomone Labs ICA-27243 modulate KCNQ2/KCNQ3 voltage-gated K+ currents expressed in Xenopus oocytes.
    A. Time course of KCNQ2/KCNQ3 current enhancement by 2 and 10 µM ICA-27243 (#I-130) as measured at -25 mV. Currents were elicited by application of voltage ramp from a holding potential of -100 mV to 0 mV (800 msec).
    B. Superimposed example traces of current responses before and during perfusion of 10 µM ICA-27243 as indicated.
    References - Scientific Background
    1. Wickenden, A.D. et al. (2008) Mol. Pharmacol. 73, 977.
    Scientific background KCNQ2 (KV7.2) and KCNQ3 (KV7.3) are voltage-gated K+ channel subunits that underlie the neuronal M current. ICA-27243 is a novel, potent and selective activator of M-current and KCNQ2/Q3 channels. ICA-27243 is structurally distinct from other known KCNQ/M-current activators. It enhances KCNQ channel activation by shifting channel opening to more hyperpolarized potentials. ICA-27243 activates KCNQ currents in Chinese hamster ovary cells expressing recombinant KCNQ2/Q3 heteromultimeric channels with an EC50 of 0.4 μM. ICA-27243 exhibits selectivity for KCNQ2/Q3 over KCNQ4 (20-fold) and KCNQ3/Q5 (>100-fold) and has no effect on GABA-activated chloride channels, neuronal Na+ channels, or voltage-gated Ca2+ channels. In addition, it produces minimal displacement of radioligand binding to a range of central nervous system receptors and transporters. ICA-27243 also suppresses seizure-like activity in an ex vivo hippocampal slice model, and protects against maximal electroshock-induced seizures in mice1.
    Target KCNQ2, KCNQ3 K+ channels
    Last update: 03/03/2019

    ICA-27243 (#I-130) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use