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NS 11021

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Chemical Structure| 956014-19-0 同义名 : -
CAS号 : 956014-19-0
货号 : A548086
分子式 : C16H9BrF6N6S
纯度 : 95%
分子量 : 511.242
MDL号 : MFCD24387114
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(205.38 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Calcium-activated potassium channels of the KCa1.1 class are known to regulate repolarization of action potential discharge through a molecular association with high voltage-activated calcium channels[1]. Inhibiting the function of KCa1.1 in healthy myoblasts induced an increase in cytosolic calcium levels and altered nuclear factor kappa B (NFκB) levels without affecting cell survival. In these normal cells, KCa1.1 block resulted in enhanced proliferation and decreased matrix metalloproteinase secretion, migration, and myotube fusion, phenotypes all observed in DM1 myoblasts and associated with disease pathogenesis. In contrast, introducing functional KCa1.1 α-subunits into DM1 myoblasts normalized their proliferation and rescued expression of the late myogenic marker Mef2[2]. K(Ca)1.1 WT and KO mice displayed identical FSK and CCH-stimulated Isc changes, indicating that K(Ca)1.1 channels are not involved in FSK- and cholinergic-stimulated Cl- secretion. CCH-stimulated DeltaIsc was significantly reduced in K(Ca)3.1 KO mice, underscoring the known relevance of this channel in the activation of Cl- secretion by an intracellular Ca2+ increasing agonist. The residual CCH effect observed in K(Ca)3.1 KO mice suggests that yet another K+ channel is driving the CCH-stimulated Cl- secretion. In the presence of the specific K(V)7.1 channel blocker 293B, the residual CCH effect was abolished[3].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[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.96mL

0.39mL

0.20mL

9.78mL

1.96mL

0.98mL

19.56mL

3.91mL

1.96mL
参考文献

[1]Renata Rehak,et al. Low voltage activation of KCa1.1 current by Cav3-KCa1.1 complexes. PLoS One. 2013 Apr 23;8(4):e61844.

[2] Rajeev B Tajhya,et al. Functional KCa1.1 channels are crucial for regulating the proliferation, migration and differentiation of human primary skeletal myoblasts. Cell Death Dis. 2016 Oct 20;7(10):e2426.

[3]J E Matos,et al. Role of cholinergic-activated KCa1.1 (BK), KCa3.1 (SK4) and KV7.1 (KCNQ1) channels in mouse colonic Cl- secretion. Acta Physiol (Oxf). 2007 Mar;189(3):251-8.

[4] Bentzen BH, 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.