NS-1619

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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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