CGP37157 是一种 Na+/Ca2+ 交换抑制剂，抑制 Na+ 诱导的豚鼠心脏线粒体中 Ca2+ 的释放，IC50 为 0.8 μM。

CGP37157 is a Na+/Ca2+ exchanger inhibitor, inhibits Na+-induced Ca2+ release from mitochondria in guinea pig heart with IC50 of 0.8 μM.

Administration of 10?μM CGP37157 shows an inhibitory effect on mitochondrial Na+/Ca2+ exchanger in cortical neurons, modulating intracellular Ca2+ levels via suppressing voltage-gated calcium channels. Administration of 10?μM CGP37157 in combination with salinomycin significantly attenuates cell viability and increases apoptosis of FaDu and HLaC79 cells. CGP37157 has no inhibitory effect on salinomycin tumor toxicity[2]. Administration of 10?μM CGP37157 reduces NMDA-induced cytosolic and mitochondrial Ca2+ overloads and it also reduces NMDA-induced excitotoxicity, and such an effect is via attenuating mitochondrial damage and calpain activity in neurons[3].

75450-34-9

C15H11Cl2NOS

324.23

7-Chloro-5-(2-chlorophenyl)-1,5-dihydro-4,1-benzothiazepine-2(3H)-one

DMSO:65 mg/mL (200.48 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years