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