BUY KC 12291 hydrochloride

KC 12291 hydrochloride

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 established.
KC 12291 is an orally active atypical voltage-gated sodium channel blocker with cardioprotective properties. 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 heart.
KC 12291 abolishes diastolic contracture in isolated myocytes obtained from guinea-pig atria, with IC₅₀ values of 0.55 and 0.79 uM, respectively and the IC₅₀ for KC 12291 inhibition of the sustained component of Na⁺current, INaL, is 9.6 uM.
KC 12291 exerts a potent bradycardic effect in the rat.