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NS6180

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Chemical Structure| 353262-04-1 同义名 : -
CAS号 : 353262-04-1
货号 : A401163
分子式 : C16H12F3NOS
纯度 : 99%+
分子量 : 323.333
MDL号 : MFCD01833144
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(324.74 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.09mL

0.62mL

0.31mL

15.46mL

3.09mL

1.55mL

30.93mL

6.19mL

3.09mL
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