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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

用途

NS-1619是 Ca2_addition_-activated K_addition_-channel选择性激动剂。

名称

[ CAS 号 ]:
153587-01-0

[ 中文名 ]:
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

[ 英文名 ]:
NS-1619

[英文别名 ]:

Lopac-N-170
NS-1619

生物活性

[ 描述 ]:

NS-1619是 Ca2_addition_-activated K_addition_-channel选择性激动剂。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> 钾通道

研究领域 >> 心血管疾病

[参考文献]

[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.

[相关活性小分子]

物理化学性质

[ 密度 ]:
1.563g/cm3

[ 熔点 ]:
234 °C(dec.)

[ 分子式 ]:
C₁₅H₈F₆N₂O₂

[ 分子量 ]:
362.22700

[ 精确质量 ]:
362.04900

[ PSA ]:
58.02000

[ LogP ]:
4.06200

[ 外观性状 ]:
固体;White to Almost white powder to crystaline

[ 折射率 ]:
1.538

[ 储存条件 ]:
存放于惰性气体之中;避免空气

MSDS

详细MSDS(安全技术说明书)

安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危险品运输编码 ]:
NONH for all modes of transport

[ 海关编码 ]:
2933990090

海关

[ 海关编码 ]: 2933990090

[ 中文概述 ]:
2933990090. 其他仅含氮杂原子的杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

文献

Potassium channel openers prevent palmitate-induced insulin resistance in C2C12 myotubes.

Arch. Biochem. Biophys. 541 , 47-52, (2014)

Insulin resistance (IR) of muscle cells is an early symptom of type 2 diabetes. It often results from excessive lipid accumulation in muscle fibers which under in vitro experimental conditions may be ...

Potassium ion channels and allergic asthma.

Adv. Exp. Med. Biol. 838 , 35-45, (2015)

High-conductive calcium-sensitive potassium channels (BK+Ca) and ATP-sensitive potassium (K+ATP) channels play a significant role in the airway smooth muscle cell and goblet cell function, and cytokin...

High glucose alters apoptosis and proliferation in HEK293 cells by inhibition of cloned BK Ca channel.

J. Cell Physiol. 226(6) , 1660-75, (2011)

It has been reported that diabetic vascular dysfunction is associated with impaired function of large conductance Ca(2+) -activated K(+) (BK(Ca) ) channels. However, it is unclear whether impaired BK(...

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