CGP37157 is a potent, selective inhibitor of Na/Ca exchanger, inhibiting the Na-induced Ca-release from guinea-pig heart mitochondria, with an IC50 of 0.8 μM.
IC50&Target
IC50: 0.8 μM (Na/Ca exchanger)
体外研究
CGP37157 (Compound XVI) is a potent, selective inhibitor of Na/Ca exchanger, inhibiting the Na-induced Ca-release from guinea-pig heart mitochondria, with an IC50 of 0.8 μM. CGP37157 (10 μM) shows inhibitory effect on mitochondrial Na/Ca exchanger in cortical neurons, modulates intracellular Ca levels via suppresssing voltage-gated calcium channels, and reduces NMDA-induced cytosolic and mitochondrial Ca overloads. CGP37157 (10 μM) also reduces NMDA-induced excitotoxicity, and such an effect is via attenuating mitochondrial damage and calpain activity in neurons. CGP37157 (10 μM) in combination with salinomycin significantly attenuates cell viability and increases apoptosis of FaDu and HLaC79 cells. Moreover, CGP37157 has no inhibitory effect on salinomycin tumor toxicity.
分子式
C15H11NOscl2
分子量
324.22
CAS号
75450-34-9
运输条件
Room temperature in continental US; may vary elsewhere.