The current application relates to compounds that bind and inhibit the inactivation of Navi.5 voltage-gated sodium channel (VGSC). The compounds can be used for treating cardiovascular diseases such as Brugada syndrome, cardiac arrhythmia disorder, progressive cardiac conduction disorder (PCCD), sick sinus syndrome, progressive familial block, atrial fibrillation, sudden infant death syndrome, dilated cardiomyopathy, myocardial ischemia/infarction, or heart failure.