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CAS No.: 353262-04-1

NS6180 Catalog No. CSN18234

Synonyms: N/A

NS-6180 is a channel blocker of KCa3.1 (IC50= 9 nM for rat and 14 nM for human). It can prevent T-cell activation and inflammation.

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生物活性

实验方案

技术信息

生物活性

描述NS6180 is a novel potent and selective KCa3.1 channel inhibitor (IC50 = 9 nM) preventing T-cell activation and inflammation. NS6180 inhibited endogenously expressed K(Ca) 3.1 channels in human, mouse and rat erythrocytes, with similar potencies (15-20 nM). NS6180 suppressed rat and mouse splenocyte proliferation at submicrolar concentrations and potently inhibited IL-2 and IFN-γ production, while exerting smaller effects on IL-4 and TNF-α and no effect on IL-17 production. Despite poor plasma exposure, NS6180 (3 and 10 mg/kg b.i.d.) dampened colon inflammation and improved body weight gain as effectively as the standard IBD (inflammatory bowel disease) drug sulfasalazine (300 mg/kg q.d.)^[3].
参考文献

[1] Jorgensen S, Dyhring T, et al. A high-throughput screening campaign for detection of ca(2+)-activated k(+) channel activators and inhibitors using a fluorometric imaging plate reader-based tl(+)-influx assay. Assay Drug Dev Technol. 2013 Apr;11(3):163-72.
[2] Strobæk D, Brown DT, et al. NS6180, a new K(Ca) 3.1 channel inhibitor prevents T-cell activation and inflammation in a rat model of inflammatory bowel disease. Br J Pharmacol. 2013 Jan;168(2):432-44.
[3] Strøbæk D, Brown DT, Jenkins DP, et al. NS6180, a new K(Ca) 3.1 channel inhibitor prevents T-cell activation and inflammation in a rat model of inflammatory bowel disease. Br J Pharmacol. 2013;168(2):432-444

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.0928 mL
- 15.4639 mL
- 30.9279 mL
- 5 mM
- 0.6186 mL
- 3.0928 mL
- 6.1856 mL
- 10 mM
- 0.3093 mL
- 1.5464 mL
- 3.0928 mL

技术信息

CAS号

353262-04-1

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C16H12F3NOS

运输

蓝冰

分子量

323.33

别名

N/A

溶解度

DMSO	120.0 mg/mL (371.1 mM)
Water	insoluble

动物实验配方

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