KC 12291 hydrochloride

Non Antibodies

NaV channels

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

449, 99

An Orally Effective Cardioprotective NaV Channel Blocker

DMSO. Centrifuge all product preparations before use (10000 x g 5 min).

41116134

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.

Yes

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.