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XE991 dihydrochloride

A Blocker of KCNQ Channels

Cat #: X-101
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 449.37
    Purity: >98%
    Form Lyophilized powder.
    Effective concentration 0.1-300 µM.
    Chemical name 10,10-bis(4-Pyridinylmethyl)-9(10H)-anthracenone dihydrochloride.
    Molecular formula C26H22Cl2N2O.
    CAS No.: 122955-13-9
    Activity XE991 blocks KCNQ channels with IC50 of 0.5-10 µM1.
    1. Wang, H.S. et al. (2000) Mol. Pharmacol. 57, 1218.
    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 Up to 50mM in water. Mild warming or agitation may be required. Spin-down all product preparations before handling.
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
    Our bioassay
    • Alomone Labs XE991 dihydrochloride blocks KCNQ2/KCNQ3 channels heterologously expressed in Xenopus oocytes.
      Alomone Labs XE991 dihydrochloride 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 dihydrochloride (#X-101) inhibits the KCNQ2/KCNQ3 current in a reversible manner (indicated by the horizontal bar). B. Representative current traces before and during application of 100µM XE991 dihydrocloride 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
    Image & Title XE991 dihydrochloride
    Alomone Labs XE991 dihydrochloride inhibits KCNQ currents in mouse dorsal raphe nucleus neurons.Sample time course shows that KCNQ currents are completely blocked by 3 µM XE991 dihydrochloride (#X-101).Adapted from Zhao, C. et al. (2017) Front. Cell. Neurosci. 11, 405. with permission of Frontiers.
    Last update: 12/08/2021

    XE991 dihydrochloride (#X-101) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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