Kv1.5-IN-1 is a selective inhibitor of the Kv1.5 potassium channel, exhibiting an IC50 value of 0.51 μM in humanKv1.5 channels. The introduction of a methoxy group at the R5 position maintains its inhibitory potency while demonstrating enhanced selectivity—approximately 2,600-fold over compound Ik and 300-fold over compound IId. This high selectivity profile suggests a favorable safety margin, promoting further pharmacodynamic and pharmacokinetic studies. Kv1.5-IN-1 is promising for research into therapies targeting diseases associated with dysfunctional Kv1.5 channel activity.
Kv1.5-IN-1 is a selective inhibitor of the Kv1.5 potassium channel, exhibiting an IC50 value of 0.51 μM in humanKv1.5 channels. The introduction of a methoxy group at the R5 position maintains its inhibitory potency while demonstrating enhanced selectivity—approximately 2,600-fold over compound Ik and 300-fold over compound IId. This high selectivity profile suggests a favorable safety margin, promoting further pharmacodynamic and pharmacokinetic studies. Kv1.5-IN-1 is promising for research into therapies targeting diseases associated with dysfunctional Kv1.5 channel activity.
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