IC50: 0.8 μM (Na ⁺ /Ca ²⁺ exchanger)

CGP37157 (Compound XVI) is a potent, selective inhibitor of Na ⁺ /Ca ²⁺ exchanger, inhibiting the Na ⁺ -induced Ca ²⁺ -release from guinea-pig heart mitochondria, with an IC ₅₀ of 0.8 μM. CGP37157 (10?μM) shows inhibitory effect on mitochondrial Na ⁺ /Ca ²⁺ exchanger in cortical neurons, modulates intracellular Ca ²⁺ levels via suppresssing voltage-gated calcium channels, and reduces NMDA-induced cytosolic and mitochondrial Ca ²⁺ 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.