Ranolazine
Selective sodium channel blocker / Ranolazine is an FDA-approved drug used for the treatment of chronic angina. It inhibits the late inward sodium current in heart muscle leading to decreased intracellular calcium levels.1 It blocks Nav 1.4, 1.5, 1.7 and 1.8 (IC50’s = 2.42, 6.22, 1.72(10.33), 21.53 µM respectively.
Biochemicals & reagents
142387-99-3
1) Belardinelli, et al., (2006), Inhibition of the late sodium current as a potential cardioprotective principle: effects of the late sodium current inhibitor ranolazine; Heart 92 iv6 2) Wang, et al. (2008), State- and Use-Dependent Block of Muscle Nav1.4 and Neuronal Nav1.7 Voltage-Gated Na+-Channel Isoforms by Ranolazine; Mol. Pharmacol. 73 940 3) Rajamani, et al., (2008), Block of tetrodotoxin-sensitive, Na(V)1.7 and tetrodotoxin-resistant, Na(V)1.8, Na+ channels by ranolazine; Channels(Austin) 2 449
RT
TARGET: Ion channel -- PATHWAY: Calcium signaling; Sodium channel -- DISEASE AREA: Heart disease; Diabetes