SERCA2a activator 1

SERCA2a activator 1 (Compound A) is a sarco/endoplasmic reticulum Ca 2+ -dependent ATPase 2a (SERCA2a) activator. SERCA2a activator 1 attenuates phospholamban inhibition and enhances the systolic and diastolic functions of the heart. SERCA2a activator 1 can be used for heart failure In Vitro SERCA2a activator 1 (Compound A) activates the Ca 2+ -dependent ATPase activity of cardiac sarcoplasmic reticulum (SR) vesicles but not that of skeletal muscle SR vesicles that lack phospholamban (PLN). 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. SERCA2a activator 1 also increases the Ca 2+ transients and contraction and relaxation of isolated adult rat cardiomyocytes. In isolated perfused rat hearts, the SERCA2a activator 1 enhances systolic and diastolic functions. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo SERCA2a activator 1 (Compound A; 30mg/kg; intravenous injection; male Wistar rats) treatment significantly enhances the diastolic function in anesthetized normal rats . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Wistar rats (7-8 weeks old) Dosage: 30mg/kg Administration: Intravenous injection Result: Significantly enhanced the diastolic function in anesthetized normal rats. Form:Solid IC50& Target:SERCA2a

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