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Merck
CN

N170

NS 1619

powder

别名:

1,3-二氢-1- [2-羟基-5-(三氟甲基)苯基]-5-(三氟甲基)-2H-苯并咪唑-2-酮

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关于此项目

经验公式(希尔记法):
C15H8F6N2O2
化学文摘社编号:
分子量:
362.23
NACRES:
NA.32
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
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产品名称

NS 1619, powder

InChI

1S/C15H8F6N2O2/c16-14(17,18)7-1-3-10-9(5-7)22-13(25)23(10)11-6-8(15(19,20)21)2-4-12(11)24/h1-6,24H,(H,22,25)

SMILES string

Oc1ccc(cc1N2C(=O)Nc3cc(ccc23)C(F)(F)F)C(F)(F)F

InChI key

YLFMCMWKHSDUCT-UHFFFAOYSA-N

form

powder

color

white

solubility

45% (w/v) aq 2-hydroxypropyl-β-cyclodextrin: 0.47 mg/mL
ethanol: 26.6 mg/mL
0.1 M NaOH: 5.2 mg/mL
DMSO: 5.3 mg/mL
H2O: insoluble

Quality Level

Gene Information

mouse ... Kcnma1(16531)
rat ... Kcnma1(83731)

Application

NS 1619 已被用作钙激活钾通道(BK)-激活剂:研究其对小鼠胸主动脉环的血管舒张作用,评估其对骨骼肌肌浆/内质网Ca2+-ATP酶(SERCA)活性的作用,测定其对小鼠脑肿瘤微血管内皮细胞中caveolin-1 蛋白表达的作用

Biochem/physiol Actions

NS 1619 是选择性大电导 Ca 2+ 激活的 K + 通道激活剂。该化合物以其血管扩张属性抗增殖特性而闻名。研究表明,NS 1619 对心肌缺血再灌注损伤具有保护作用。
NS-1619可以促进心肌细胞中线粒体活性氧(ROS)的形成。它可增加培养的脑片中ROS的形成。NS-1619具有增强野生型(WT)动物中HO-1活性的能力。

Disclaimer

光敏性

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

Eyeshields, Gloves, type N95 (US)


历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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Preconditioning with the BKCa channel activator NS-1619 prevents ischemia-reperfusion-induced inflammation and mucosal barrier dysfunction: roles for ROS and heme oxygenase-1
Dai H, et al.
American Journal of Physiology. Heart and Circulatory Physiology, 313(5), H988-H999 (2017)
G Edwards et al.
British journal of pharmacology, 113(4), 1538-1547 (1994-12-01)
1. The effects of NS 1619, the putative BKCa channel opener, were investigated on rat intact portal veins and on single smooth muscle cells enzymatically separated from the same tissue. 2. Under whole-cell patch clamp conditions with K-rich pipettes, exposure
BK channel activation by NS-1619 is partially mediated by intracellular Ca2+ release in smooth muscle cells of porcine coronary artery
Hisao Yamamura
British Journal of Pharmacology (2001)
Vincenzo Calderone et al.
Naunyn-Schmiedeberg's archives of pharmacology, 375(1), 73-80 (2007-01-05)
Large-conductance calcium-activated potassium channels (BK) of smooth muscle play a role in the relevant modulation of vascular tone, due to their calcium- and voltage-dependent mechanisms of activation. A potential role of endothelial BK channels has also been suggested by approaches
Yajun Liu et al.
American journal of physiology. Gastrointestinal and liver physiology, 302(1), G44-G54 (2011-09-17)
The objectives of this study were to determine whether neutrophil depletion with anti-neutrophil serum (ANS) or preconditioning with the hydrogen sulfide (H(2)S) donor NaHS (NaHS-PC) 24 h prior to ischemia-reperfusion (I/R) would prevent postischemic mitochondrial dysfunction in rat intestinal mucosa

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