CGP37157

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. IC50 & Target: IC50: 0.8 μM (Na⁺/Ca²⁺ exchanger)^[1] In Vitro: CGP37157 (Compound XVI) 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^[1]. CGP37157 (10 μM) shows inhibitory effect on mitochondrial Na⁺/Ca²⁺ exchanger in cortical neurons, modulates intracellular Ca²⁺ levels via suppresssing voltage-gated calcium channels, and reduces NMDA-induced cytosolic and mitochondrial Ca²⁺ overloads. CGP37157 (10 μM) also reduces NMDA-induced excitotoxicity, and such an effect is via attenuating mitochondrial damage and calpain activity in neurons^[2]. 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^[3].