NS 1619
(Synonyms: 1-(2-羟基-5-(三氟甲基)苯基)-5-(三氟甲基)-1H-苯并[D]咪唑-2(3H)-酮) 目录号 : GC12547
A KCa1.1/BK channel opener
Cas No.:153587-01-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
NS-1619 is a selective large conductance Ca2+-activated K+-channel activator.IC50 value: Target: Ca2+-activated K+-channel activatorNS 1619 (3-100 microM) produced a concentration-dependent inhibition of spontaneous activity in rat portal vein characterized by a reduction in the amplitude and duration of the tension waves. This inhibition was slightly potentiated in the presence of either charybdotoxin (250 nM) or penitrem A (1 microM) [1]. NS-1619 induced concentration-dependent activation of BKCa channels with a calculated EC50 of 32 microM. The NS 1619-induced activity was dependent on the presence of free Ca2+ at the intracellular surface, but was not associated with a change in channel voltage sensitivity [2]. NS 1619 (50 microM) inhibited the noradrenaline-induced contraction. NS 1619 (10-100 microM) reduced the high K+-induced contractions in a noncompetitive manner [3]. Inhalation of a 12 μM and 100 μM NS1619 solution significantly reduced RV pressure without affecting systemic arterial pressure. Blood gas analyses demonstrated significantly reduced carbon dioxide and improved oxygenation in NS1619-treated animals pointing towards a considerable pulmonary shunt-reducing effect. In PASMC's, NS1619 (100 μM) significantly attenuated PASMC proliferation by a pathway independent of AKT and ERK1/2 activation [4].
References:
[1]. Edwards G, et al. Ion channel modulation by NS 1619, the putative BKCa channel opener, in vascular smooth muscle. Br J Pharmacol. 1994 Dec;113(4):1538-47.
[2]. Lee K, et al. NS 1619 activates BKCa channel activity in rat cortical neurones. Eur J Pharmacol. 1995 Jul 4;280(2):215-9.
[3]. Huang Y, et al. NS 1619 activates Ca2+-activated K+ currents in rat vas deferens. Eur J Pharmacol. 1997 Apr 23;325(1):21-7.
[4]. Revermann M, et al. Inhalation of the BK(Ca)-opener NS1619 attenuates right ventricular pressure and improves oxygenation in the rat monocrotaline model of pulmonary hypertension. PLoS One. 2014 Jan 31;9(1):e86636.
| Cas No. | 153587-01-0 | SDF | |
| 别名 | 1-(2-羟基-5-(三氟甲基)苯基)-5-(三氟甲基)-1H-苯并[D]咪唑-2(3H)-酮 | ||
| 化学名 | 1-(2-hydroxy-5-(trifluoromethyl)phenyl)-5-(trifluoromethyl)-1H-benzo[d]imidazol-2(3H)-one | ||
| Canonical SMILES | FC(F)(C1=CC=C(C(NC2=O)=C1)N2C(C=C(C(F)(F)F)C=C3)=C3O)F | ||
| 分子式 | C15H8F6N2O2 | 分子量 | 362.23 |
| 溶解度 | ≥ 72.4mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。