SEA0400 is a novel and selective inhibitor of the Na-Ca exchanger (NCX), inhibiting Na-dependent Ca uptake in cultured neurons, astrocytes, and microglia with IC50s of from 5 to 33 nM.
IC50&Target
IC50: 5-33 nM (NCX)
体外研究
SEA0400 inhibits Na-dependent Ca uptake in cultured neurons, astrocytes, and microglia. IC50 values of SEA0400 are 33 nM (neurons), 5.0 nM (astrocytes), and 8.3 nM (microglia). SEA0400 prevents sodium nitroprusside (SNP) to increase ERK and p38 MAPK phosphorylation, and production of reactive oxygen species (ROS) in an extracellular Ca-dependent manner.
体内研究
SEA0400 (3 mg/kg + 3 mg/kg/h for 2 h, i.v.) attenuates the infarct volume in the cerebral cortex and striatum, does not affect the mean the regional cortical blood flow in anesthetized rats. SEA0400 protects against the dopaminergic neurotoxicity (determined by dopamine levels in the midbrain and striatum, tyrosine hydroxylase immunoreactivity in the substantia nigra and striatum, striatal dopamine release, and motor deficits) in MPTP-treated C57BL/6J mice.
分子式
C21H19F2NO3
分子量
371.38
CAS号
223104-29-8
运输条件
Room temperature in continental US; may vary elsewhere.