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A Potent and Selective Opener of KCNQ2 and KCNQ3 K+ Channels

Cat #: I-130
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 268.64
    Purity: >99%
    Effective concentration 0.5-50 µM.
    Chemical name N-(6-Chloro-pyridin-3-yl)-3,4-difluoro-benzamide.
    Molecular formula C12H7ClF2N2O.
    CAS No.: 325457-89-4
    PubChem CID 9903497
    Activity ICA-27243 is a potent and selective KCNQ channel modulator (enhancer)1 with EC50 ~ 1 µM.
    1. Padilla, K. et al. (2009) Neurosci. Lett. 465, 138.
    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 100 mM DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions 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.
      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: 06/11/2022

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

    For research purposes only, not for human use
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