NS-1619

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NS-1619

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

153587-01-0

包装与价格：

包装	价格(元)
10 mM * 1 mL in DMSO	电议
5mg	电议
10mg	电议
50mg	电议
100mg	电议

产品介绍

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)。

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 EC₅₀of about 10 – 30 μM in several smooth muscles of blood vessels and other tissues^[1]. NS1619 inhibits proliferation and inducesapoptosisin A2780 ovariancancercells^[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 I_Kin human ovarian cancer cells A2780^[2].
NS1619 (10, 30, 50, and 100 μM) increases levels of p53, p21^Cip1and 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].

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 K_Cachannels with NS-1619 (1 mg/kg; i.p.) can delay protection in mouse hearts^[3].

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

性状

Solid

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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 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-CDin 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 μL20% 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本网站选购。