产品
编 号:F715122
分子式:C32H29N3O4S
分子量:551.66
产品类型
结构图
CAS No: 2139330-34-8
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产品详情
生物活性:
SERCA2a activator 1 (Compound A) is a sarco/endoplasmic reticulum Ca2+-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.
体内研究:
SERCA2a activator 1 (Compound A; 30mg/kg; intravenous injection; male Wistar rats) treatment significantly enhances the diastolic function in anesthetized normal rats.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.
体外研究:
SERCA2a activator 1 (Compound A) activates the Ca2+-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 Ca2+ transients and contraction and relaxation of isolated adult rat cardiomyocytes. In isolated perfused rat hearts, the SERCA2a activator 1 enhances systolic and diastolic functions.