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NS8593

Cat.No.:HY-137952

CASNo.:875755-39-8

分⼦式:C₁₇H₁₇N₃

分⼦量:263.34

作⽤靶点:PotassiumChannel;TRPChannel

作⽤通路:MembraneTransporter/IonChannel;NeuronalSignaling

储存⽅式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

⽣物活性NS8593是⼀种SKchannel(⼩电导钙激活钾通道)抑制剂。NS8593可逆性地抑制重组SK3介导的电流(⼈

SK3和⼤⿏SK3)。NS8593以Ca2+依赖的⽅式抑制所有SK1-3亚型(在0.5μMCa2+浓度下，Kd分别为

0.42、0.60和0.73μM)。NS8593对中等电导和⼤电导的Ca2+激活的K+通道(分别为hlk和hBK通道)没有

影响。NS8593还可以抑制TRPM7(⿊素抑制素相关TRP阳离⼦通道7)(IC50=1.6mM)。NS8593可⽤于中枢

神经系统(CNS)相关疾病的研究[1][2]。

体外研究NS8593reversiblysuppressesSK3current;IC50is91nMinHEK293cells[1].

NS8593(10μM,4min)hasnosignificanteffectonhumanIK(hIK)currentinHEK293cells[1].

NS8593s(3μM)inhibitoryeffectonHEK293cellsdecreasedwithincreasingintracellularCa2+

concentration(Kd=0.47μMat0.3μMCa2+andKd=14μMat10μMCa2+)[1].

NS8593(3μM,4min)shiftstheCa2+activationcurvetotheright(EC50increasesfrom0.43μMto1.6μM)

andreducestheHillcoefficient(from5.6to2.0)inHEK293cells[1].