KC 12291 hydrochloride

An Orally Effective Cardioprotective NaV Channel Blocker
Cat #: K-105
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 449.99
    Purity: >97%
    Effective concentration 0.5 - 100 μM.
    Chemical name 3,4-Dimethoxy-N-methyl-N-[3-[(5-phenyl-1,2,4-thiadiazol-3-yl)oxy]propyl]benzeneethanamine hydrochloride.
    Molecular formula C22H27N3O3S•HCl.
    CAS No.: 181936-98-1.
    Activity Orally active voltage-gated Na+ (NaV) channel blocker1-2 with cardioprotective properties2-4. Inhibits sustained Na+ currents (INaL) with IC50 of 9.6 μM and prevents diastolic contracture in isolated atrial myocytes (IC50 of about 0.7 μM)5.
      • Decking, U. K. et al.  (1998) Naunyn. Schmiedebergs. Arch. Pharmacol. 358, 547.

      • Hartmann, M. et al. (1998) Naunyn. Schmiedebergs. Arch. Pharmacol. 358, 554.

      • Ver Donck, L. et al. (1993) Cardiovasc. Res. 27, 349.

      • John, G.W. et al. (2004) Cardiovasc. Drug Rev. 22, 17.

      • Tamareille, S. et al. (2002) J. Cardiovasc. Pharmacol. 40, 346.

    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 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.
      • Alomone Labs KC 12291 hydrochloride inhibits NaV1.7 channels expressed in HEK293 cells.
        A. Time course of current reversible inhibition by 50 μM KC 12291 hydrochloride (#K-105). Currents were elicited by a voltage ramp from a holding potential of -100 mV to 60 mV (30 ms) delivered every 10 seconds. B. Example traces of current response to voltage ramp stimulation before and during 50 μM KC 12291 hydrochloride application.
      • Takeo, S. et al. (1995) J. Pharmacol. Exp. Ther. 273, 1403.
      • John, G. W. et al. (2004) Cardiovasc. Drug Rev. 22, 17.
      • Ver Donck, L. et al. (1993) Cardiovasc. Res. 27, 349.
      • Hartmann, M. et al. (1998) Naunyn. Schmiedebergs. Arch. Pharmacol. 358, 554.
      • Decking, U. K. et al. (1998) Naunyn. Schmiedebergs. Arch. Pharmacol. 358, 547.
      • Tamareille, S. et al. (2002) J. Cardiovasc. Pharmacol. 40, 346.
      • Létienne, R. et al. (2006) Eur. J. Pharmacol. 530, 243.
      • The pathophysiological importance of Na+ overload is highlighted by the fact that a variety of drugs reducing Na+ influx proved to be cardioprotective, both at the intact organ and cellular level. In addition, a correlation between the degree of Na+ channel blockade and functional recovery from myocardial infarction is established1.

        KC 12291 is an orally active atypical voltage-gated sodium channel blocker with cardioprotective properties2-4. It effectively blocks cardiac voltage-gated sodium channels, involving inhibition of the peak Na+ current and thus delays Na+ overload during ischemia by enhancing the inexcitability of the heart4-5.

        KC 12291 abolishes diastolic contracture in isolated myocytes obtained from guinea-pig atria, with IC50 values of 0.55 and 0.79 μM respectively, and the IC50 for KC 12291 inhibition of the sustained component of Na+ current, INaL, is 9.6 μM6.

        KC 12291 exerts a potent bradycardic effect in the rat7.

    Target NaV channels
    Last update: 03/03/2019

    KC 12291 hydrochloride (#K-105) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use