NS8593 hydrochloride 是选择性的SK通道抑制剂。它可逆抑制SK3介导的电流,Kd值为 77 nM。它抑制所有SK1-3亚型的 Ca2+依赖性 (在 0.5 μM Ca2+时,Kd分别为 0.42、0.60 和 0.73 μM),并且不影响中间电导和大电导的钙激活钾通道。
产品描述
NS8593 hydrochloride is a potent and selective inhibitor of small conductance Ca2+-activated K+ channels (SK channels) .
体外活性
It is found that tested in excised patches, the inhibition by NS8593 (compound 14) decreased as the intracellular [Ca2+] is increased and that NS8593 is equipotent when applied from either the intracellular or the extracellular side of the cell membrane.?A HEK293 cell transiently transfected with hSK3 channels is inhibited by 80% upon application of 100 nM apamin and by 75% after application of 300 nM NS8593.
体内活性
NS8593 is able to affect firing pattern and firing rate?of dopaminergic neurons in vivo in C57Bl/6 mice[1].
Cas No.
875755-24-1
分子式
C17H18ClN3
分子量
299.8
别名
NS8593 HCl
储存和溶解度
DMSO:80 mg/mL (266.84 mM,Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years