CGP37157 is a potent, selective inhibitor of Na+/Ca2+ exchanger, inhibiting the Na+-induced Ca2+-release from guinea-pig heart mitochondria, with an IC50 of 0.8 μM.
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CGP37157 is identified as a potent and selective inhibitor of the Na+/Ca2+ exchanger, particularly effective in blocking Na+-induced Ca2+-release from guinea-pig heart mitochondria at an IC50 of 0.8 μM. At a concentration of 10 μM, CGP37157 inhibits the mitochondrial Na+/Ca2+ exchanger in cortical neurons, managing intracellular Ca2+ levels by dampening voltage-gated calcium channels and mitigating NMDA-induced rises in cytosolic and mitochondrial Ca2+. Additionally, CGP37157 at this concentration diminishes NMDA-triggered excitotoxicity through the reduction of mitochondrial damage and calpain activity in neurons[2]. CGP37157 (10 μM) combined with salomycin significantly decreased the viability of FaDu and HLaC79 cells, and increased cell apoptosis. In addition, CGP37157 had no inhibitory effect on the tumor toxicity of salomycin [3].
体外研究
CGP37157 is identified as a potent and selective inhibitor of the Na+/Ca2+ exchanger, particularly effective in blocking Na+-induced Ca2+-release from guinea-pig heart mitochondria at an IC50 of 0.8 μM.
At a concentration of 10 μM, CGP37157 inhibits the mitochondrial Na+/Ca2+ exchanger in cortical neurons, managing intracellular Ca2+ levels by dampening voltage-gated calcium channels and mitigating NMDA-induced rises in cytosolic and mitochondrial Ca2+. Additionally, CGP37157 at this concentration diminishes NMDA-triggered excitotoxicity through the reduction of mitochondrial damage and calpain activity in neurons[2].
CGP37157 (10 μM) combined with salomycin significantly decreased the viability of FaDu and HLaC79 cells, and increased cell apoptosis. In addition, CGP37157 had no inhibitory effect on the tumor toxicity of salomycin [3].
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