Molecular Formula | C21H19F2NO3 |
Molar Mass | 371.38 |
Storage Condition | Keep in dark place,Inert atmosphere,Store in freezer, under -20°C |
Use | SEA0400 is a novel and selective inhibitor of Na -Ca2 + exchanger. It can inhibit Na-dependent Ca2 + absorption in cultured neurons, astrocytes and microglia with an IC50 value of 5-33 nM. |
In vitro study | SEA0400 inhibits Na + -dependent 45 Ca 2+ uptake in cultured neurons, astrocytes, and microglia. IC 50 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 2+ -dependent manner. |
In vivo study | 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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.693 ml | 13.463 ml | 26.927 ml |
5 mM | 0.539 ml | 2.693 ml | 5.385 ml |
10 mM | 0.269 ml | 1.346 ml | 2.693 ml |
5 mM | 0.054 ml | 0.269 ml | 0.539 ml |
biological activity | SEA0400 is a potent inhibitor of selective Na -Ca2 exchanger (NCX), which can inhibit Na-dependent Ca2 uptake in nerve cells, astrocytes and microglia, with corresponding IC50 values of 33 nM, 5.0 nM and 8.3 nM respectively. SEA0400 can prevent sodium nitroprusside (SNP) from increasing phosphorylation of ERK and p38 MAPK and enhancing reactive oxygen species (ROS) production in an extracellular Ca2 +-dependent manner. |
target | TargetValue p38 MAPK () ERK () ROS () NCX (in cultured astrocytes) 5.0 nM NCX (in cultured microglia) 8.3 nM |
Target | Value |
p38 MAPK () | |
ERK () | |
ROS () | |
NCX (in cultured astrocytes) | 5.0 nM |
NCX (in cultured microglia) | 8.3 nM |
in vitro study | SEA0400 inhibits Na -dependent 45 Ca 2 uptake in cultured neurons, astrocytes, and microglia. IC 50 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 2 -dependent banner. |
in vivo study | 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 nice. |