| Bioactivity | 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]. | |||||||||
| Target | Ca2+-activated big-conductance K+ Channels | |||||||||
| Invitro | 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 (mitochondrial big-conductance calcium-activated K+) 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]. | |||||||||
| Name | NS 11021 | |||||||||
| CAS | 956014-19-0 | |||||||||
| Formula | C16H9BrF6N6S | |||||||||
| Molar Mass | 511.24 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
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| Reference | [1]. Bo Hjorth Bentzen, et al. The small molecule NS11021 is a potent and specific activator of Ca2+-activated big-conductance K+ channels. Mol Pharmacol. 2007 Oct;72(4):1033-44 [2]. Cagil Coskun, et al. BK channel openers NS1619 and NS11021 reverse hydrogen peroxide-induced membrane potential changes in skeletal muscle. J Recept Signal Transduct Res. 2020 Oct;40(5):449-455. [3]. Stephen Shrum, et al. Specific BK Channel Activator NS11021 Protects Rat Renal Proximal Tubular Cells from Cold Storage-Induced Mitochondrial Injury In Vitro. Biomolecules. 2019 Dec 4;9(12):825. |
NS 11021
CAS: 956014-19-0 F: C16H9BrF6N6S W: 511.24
NS 11021 is a potent and specific Ca2+-activated big-conductance K+ Channels (KCa1.1 channels) activator. NS 11021 at co
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