NS 11021 是一种有效特异性的 Ca2+激活的大电导 K+(KCa1.1)通道激活剂。当浓度高于0.3 μM 时,NS 11021 通过平行移动通道激活曲线产生更多负电位,以浓度依赖的方式激活 KCa1.1。
生物活性 | NS 11021 is a potent and specificCa2+-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] |
体外研究 (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 inX. laevisoocytes[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 inX. laevisoocytes[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].
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 100 mg/mL(195.60 mM;Need ultrasonic) 配制储备液 1 mM | 1.9560 mL | 9.7801 mL | 19.5603 mL | 5 mM | 0.3912 mL | 1.9560 mL | 3.9121 mL | 10 mM | 0.1956 mL | 0.9780 mL | 1.9560 mL |
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此方案可获得 ≥ 2.08 mg/mL (4.07 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (4.07 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.07 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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