NS-1619

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

NS-1619  纯度: ≥98.0%

NS-1619 是 Ca2+ 激活的 K+ (BK) 通道的激活剂。 NS-1619 是一种高效的松弛剂,在血管和其他组织的几个平滑肌中的 EC50 约为 10 – 30 μM。NS1619抑制A2780卵巢癌细胞增殖并诱导细胞凋亡 (apoptosis)。

NS-1619

NS-1619 Chemical Structure

CAS No. : 153587-01-0

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10 mM * 1 mL in DMSO ¥880 In-stock
5 mg ¥800 In-stock
10 mg ¥1000 In-stock
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NS-1619 相关产品

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生物活性

NS-1619 is an opener of large conductance Ca2+-activated K+ (BK) channel. NS-1619 is a highly effective relaxant with an EC50 of about 10 – 30 μM in several smooth muscles of blood vessels and other tissues[1]. NS1619 inhibits proliferation and induces apoptosis in A2780 ovarian cancer cells[2].

体外研究
(In Vitro)

NS1619 (5, 10, 30, 50, and 100 μM) inhibits the proliferation of A2780 cells in a dosage and time dependent manner IC50=31.1 μM for 48 h pretreatment[2].
NS1619 (30 μM) exhibits augmenting effect on whole cell IK in human ovarian cancer cells A2780[2].
NS1619 (10, 30, 50, and 100 μM) increases levels of p53, p21Cip1 and Bax proteins in A2780 cells[2].
DNA content of A2780 cells was significantly decreased after 36 and 48 h of pretreatment. The breakdown of DNA results in death of the tumor cells[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[2]

Cell Line: The human ovarian cancer cell line A2780
Concentration: 5, 10, 30, 50, and 100 μM
Incubation Time: 48 hours
Result: Inhibited cell growth in a time and concentration-dependent manner, IC50=31.1 μM.
Proliferation was significantly inhibited at concentrations of NS1619 higher than 10 μM.

Western Blot Analysis[2]

Cell Line: A2780 cells
Concentration: 0, 5, 10, 30, 50, and 100 μM
Incubation Time: 48 hours
Result: Expression of p53, p21, and Bax in A2780 cells was significantly increased in comparison with control.

Western Blot Analysis[2]

Cell Line: A2780 cells
Concentration: 30 μM
Incubation Time: 36 and 48 hours
Result: DNA content of A2780 cells was significantly decreased after 36 and 48 h of pretreatment. The breakdown of DNA results in death of the tumor cells.

体内研究
(In Vivo)

Opening of KCa channels with NS-1619 (1 mg/kg; i.p.) can delay protection in mouse hearts[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Adult male outbred ICR mice[3]
Dosage: 1 mg/kg
Administration: Pretreated i.p. 24 h before I/R
Result: Pretreatment induced delayed protection 24 h later.
Resulted in significant cardioprotection 24 h later, i.e., infarct size was reduced from 38.8 ± 3.7% to 19.8 ± 2.9%.

分子量

362.23

Formula

C15H8F6N2O2

CAS 号

153587-01-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 31 mg/mL (85.58 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7607 mL 13.8034 mL 27.6068 mL
5 mM 0.5521 mL 2.7607 mL 5.5214 mL
10 mM 0.2761 mL 1.3803 mL 2.7607 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 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,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制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

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.90 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.90 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 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。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.90 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.90 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. H Yamamura, et al. BK channel activation by NS-1619 is partially mediated by intracellular Ca2+ release in smooth muscle cells of porcine coronary artery. Br J Pharmacol. 2001 Feb;132(4):828-34.

    [2]. Xiaobing Han,et al. The potassium ion channel opener NS1619 inhibits proliferation and induces apoptosis in A2780 ovarian cancer cells. Biochem Biophys Res Commun. 2008 Oct 17;375(2):205-9.

    [3]. Xiaoyin Wang, et al. Opening of Ca2+-activated K+ channels triggers early and delayed preconditioning against I/R injury independent of NOS in mice. Am J Physiol Heart Circ Physiol. 2004 Nov;287(5):H2070-7.

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