NS 6180
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IC50:作用于大鼠、人和小鼠红细胞KCa3.1通道的IC50分别为9、14和15 nM。
NS 6180是一种强效的KCa3.1通道阻断剂。KCa3.1(Ca2+激活的K+通道,由KCNQ4基因编码)通过参与调节钙进入在这些过程中起关键作用。
体外:NS6180通过T250和V275阻断克隆的人KCa3.1通道,而相同的氨基酸残基赋予三芳基甲烷如TRAM-34敏感性。NS6180以相似效力阻断内源性表达的人、小鼠和大鼠红细胞KCa3.1通道。亚微摩尔浓度的NS6180可抑制大鼠和小鼠脾细胞增殖,强效抑制IL-2和IFN-g的产生,对IL-4和TNF-a具有较小的作用,对IL-17的产生无影响。诱导结肠炎后,在健康结肠中抗体染色表明,与浸润免疫细胞相关的KCa3.1通道强烈上调[1]。
体内:如标准IBD药物柳氮磺胺吡(300 mg·kg-1 q.d.),尽管血浆暴露差,NS6180(3和10 mg·kg-1 b.i.d.)消除结肠炎症并有效改善体重增加。苯并噻嗪NS6180对重组和内源性表达的KCa3.1通道均有效。此外,NS6180的效果表征其对野生型和KCa3.1–/–敲除小鼠T淋巴细胞活性的药代动力学,并表明其消除IBD动物模型的炎症[1]。
临床试验:目前尚未进行临床研究。
参考文献:
[1] Strbk D, Brown DT, Jenkins DP, Chen YJ, Coleman N, Ando Y, Chiu P, Jrgensen S, Demnitz J, Wulff H, Christophersen P. 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.
Storage | Store at -20°C |
M.Wt | 323.33 |
Cas No. | 353262-04-1 |
Formula | C16H12F3NOS |
Solubility | Soluble in DMSO |
Chemical Name | 4-(3-(trifluoromethyl)benzyl)-2H-benzo[b][1,4]thiazin-3(4H)-one |
SDF | Download SDF |
Canonical SMILES | FC(F)(C1=CC(CN2C3=CC=CC=C3SCC2=O)=CC=C1)F |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |