SERCA2a activator 1 activates the Ca2+-dependent ATPase activity of cardiac sarcoplasmic reticulum vesicles but not that of skeletal muscle SR vesicles that lack phospholamban. SERCA2a activator 1 also increases the Ca2+ transients and contraction and relaxation of isolated adult rat cardiomyocytes. The surface plasmon resonance assay reveals a direct interaction between SERCA2a activator 1 and PLN, suggesting that the binding of SERCA2a activator 1 to PLN attenuates its inhibition of SERCA2a, resulting in SERCA2a activation [1].

SERCA2a activator 1 (30mg/kg; intravenous injection; male Wistar rats) treatment obviously increases the diastolic function in anesthetized normal rats [1].