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NS 11021 {[allProObj[0].p_purity_real_show]}

货号:A548086

NS 11021是一种强效且特异性的 KCa1.1 通道激活剂,在浓度高于 0.3 μM 时通过激活通道产生负电位。

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Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
NS 11021 化学结构 CAS号:956014-19-0
NS 11021 化学结构
CAS号:956014-19-0
NS 11021 3D分子结构
CAS号:956014-19-0
NS 11021 化学结构 CAS号:956014-19-0
NS 11021 3D分子结构 CAS号:956014-19-0
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NS 11021 纯度/质量文件 产品仅供科研

货号:A548086 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Potassium Channel 其他靶点 纯度
Tolbutamide 98%
Glimepiride ++++

SUR1, IC50: 5.4 nM

SUR2B, IC50: 7.3 nM

97%
Dronedarone HCl 95%
Gliquidone ++

Potassium channel, IC50: 27.2 nM

99%
TRAM-34 +++

IKCa1 (KCa3.1), Kd: 20 nM

98%
Glibenclamide 98%
Amiodarone HCl 97%
Gliclazide ++

Potassium channel, IC50: 184 nM

98%
Repaglinide 98%
Dofetilide 98%
Nateglinide 99%
Quinine HCl dihydrate 98%
ML133 HCl +

Kir2.1, IC50: 290 nM

99%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

NS 11021 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].

NS 11021 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.

NS 11021 实验方案

计算器
存储液制备 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

NS 11021 技术信息

CAS号956014-19-0
分子式C16H9BrF6N6S
分子量 511.24
SMILES Code S=C(NC1=CC=C(Br)C=C1C2=NNN=N2)NC3=CC(C(F)(F)F)=CC(C(F)(F)F)=C3
MDL No. MFCD24387114
别名
运输蓝冰
InChI Key MDKAFDIKYQMOMF-UHFFFAOYSA-N
Pubchem ID 24825677
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry, 2-8°C

溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案一
方案二
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