XE991

A Blocker of KCNQ Channels
    Cat #: X-100
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 376.45
    Purity: >95%
    Formulation Lyophilized powder.
    Effective concentration 0.1-300 µM.
    Structure
    Chemical name 10,10-bis(4-Pyridinylmethyl)-9(10H)-anthracenone.
    Molecular formula C26H20N2O.
    CAS No.: 122955-42-4.
    References - Activity
    1. Wang, H.S. et al. (2000) Mol. Pharmacol. 57, 1218.

    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 in DMSO. Centrifuge all product preparations before use (10000 x g 1 min).
    Storage after reconstitution Up to four weeks at 4°C or three months at -20°C.
    Our bioassay
    Alomone Labs XE991 blocks KCNQ2/KCNQ3 channels heterologously expressed in Xenopus oocytes.
    A. Time course of KCNQ2/KCNQ3 maximal current amplitude, elicited by 700 ms voltage step from holding potential of -100 mV to -30 mV, delivered every 10 seconds. Application of 100 µM XE991 (#X-100) inhibits the KCNQ2/KCNQ3 current in a reversible manner (indicated by the horizontal bar). B. Representative current traces before and during application of 100 µM XE991 as indicated.
    References - Scientific Background
    1. Yeung, S.Y. and Greenwood, I.A. (2005) Br J Pharmacol146, 585.
    2. Zaczek, R. et al. (1998) Pharmacol. Exp. Ther. 285, 724.
    3. Fontán-Lozano, A. et al. (2009) Hippocampus 21, 22.
    Scientific background

    Voltage-gated K+ channels of the KCNQ family (KV7) are widely expressed in nerves and smooth muscles where their general role is to hyperpolarise the cell membrane and thereby dampen excitability1.

    XE991 is a potent and selective blocker of KCNQ voltage-gated K+ channels. It blocks KV7.2 + KV7.3 (KCNQ2 + KCNQ3)/M-currents (IC50 = 0.6 μM) and KV7.1 (KCNQ1) homomeric channels (IC50 = 0.75 μM) but is less potent against KV7.1/minK channels (IC50 = 11.1 μM)1. Suppression of the M-current causes an increase in intrinsic excitability2. XE991 enhances acetylcholine release from rat brain slices (EC50 = 490 nM) and shows good in vivo potency and duration of action, suggesting utility in Alzheimer’s disease therapeutics2. It was demonstrated that XE991 enhances learning and memory in healthy mice3.

    Target KCNQ K+ channels
    Last update: 14/01/2019

    XE991 (#X-100) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
    Citations
    Product citations
    1. Muqeem, T. et al. (2018) J. Neurosci. 38, 3729.
    2. Nassoiy, S.P. et al. (2017) J. Biomed. Sci. 24, 8.
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