S89252 |
NS-11021 |
源叶(MedMol) | 98% |
- 产品描述: 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
- 靶点: Ca2+-activated big-conductance K+ Channels;PotassiumChannel
- 体外研究:
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. 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. NS 11021 (0-10 μM) can enhance hKCa1.1 currents in a concentration-dependent manner in monoclonal HEK293 cells stably expressing hKCa1.1. 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. 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
- 参考文献:
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.
- 溶解性: Soluble in DMSO
- 保存条件: 2-8°C
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 1.956 ml 9.78 ml 19.56 ml 5 mM 0.391 ml 1.956 ml 3.912 ml 10 mM 0.196 ml 0.978 ml 1.956 ml 50 mM 0.039 ml 0.196 ml 0.391 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)