NS 11021

NS 11021 is a potent and specific Ca²⁺-activated big-conductance K⁺ Channels (KCa1.1 channels) activator. NS 11021 at concentrations above 0.3 μM activates KCa1.1 in a concentration-dependent manner by parallelshifting the channel activation curves to more negative potentials^[1]. IC50 & Target:Ca²⁺-activated big-conductance K⁺ Channels^[1] In Vitro:NS 11021 (1-30 μM) increases the current of hKCa1.1 from 2 μA to 4 μA at the concentration of 3 μM and can activate the hKCa1.1 expression channel in a dose-dependent manner in X. laevis oocytes^[1].
NS 11021 (3 μM) increases hKCa1.1 current for channels by 171 % which repeatedly shifts between open and closed structures while increases the hKCa1.1 current by 187 % for channels kept in closed conformation in X. laevis oocytes^[1].
NS 11021 (0-10 μM) can enhance hKCa1.1 currents in a concentration-dependent manner in monoclonal HEK293 cells stably expressing hKCa1.1^[1].
NS 11021 (5 or 50 μM) has no effect on resting membrane potential (RMP), while significantly increasing action potential (AP) rise time in a dose-dependent manner in frogs gastrocnemius muscles. NS 11021 completely reverses the deleterious effects of hydrogen peroxide on the AP repolarization phase in skeletal muscle fibers^[2].
NS 11021 (1 μM) effectively attenuates mitoBK channel damage, mitochondrial respiratory dysfunction, depolarization, superoxide production and cell death induced by CS + RW (cold storage (18 h) and rewarming (2 h)) in rat kidney proximal tubular epithelial (NRK) cells^[3].