Kv2.1-IN-1 is an orally active and blood-brain barrier penetrant Kv2.1 inhibitor with an IC 50 of 0.07 μM. Kv2.1-IN-1 exhibits a selectivity >130 fold over other K + , Na + , and Ca 2+ ion channels. Kv2.1-IN-1 decreases the apoptosis of HEK293 cells induced by H 2 O 2 . Kv2.1-IN-1 produces significant neuroprotection efficacy in middle cerebral artery occlusion (MCAO) rat. Kv2.1-IN-1 can be used for the study of ischemic stroke.
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