NS 3623

一种离子通道调节剂；抑制HEK293细胞中的VRAC和分离的人红细胞中的氯离子电导（IC50s分别为1.8和0.21µM）；激活hERG/Kv11.1（EC50=79.4µM），但在30µM时不激活Kv1.5、Kv4.3或Kv7.1；以每天100mg/kg的剂量持续21天，增加镰状细胞病SAD转基因小鼠模型中的红细胞密度并改善红细胞形态；以50mg/kg的剂量逆转清醒豚鼠中E-4031诱发的QT间期延长。An ion channel modulator; inhibits the VRAC in HEK293 cells and chloride conductance in isolated human red blood cells (IC50s = 1.8 and 0.21 µM, respectively); activates hERG/Kv11.1 (EC50 = 79.4 µM) but does not activate Kv1.5, Kv4.3, or Kv7.1 at 30 µM; increases red blood cell density and improves red blood cell morphology in the SAD transgenic mouse model of sickle cell disease at 100 mg/kg per day for 21 days; reverses E-4031-induced QT interval prolongation in conscious guinea pigs at 50 mg/kg.分子式C15H10BrF3N6O分子量427.2