SERCA2a activator 1 (Compound A) 是一种肌/内质网 Ca²⁺ 依赖性ATPase 2a (SERCA2a) 激活剂。SERCA2a activator 1 减弱了 phospholamban 抑制作用，增强了心脏的收缩和舒张功能。SERCA2a activator 1 可用于心力衰竭的研究。

SERCA2a activator 1 (Compound A) is a sarco/endoplasmic reticulum Ca-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.

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SERCA2a

SERCA2a activator 1 (Compound A) activates the Ca-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 transients and contraction and relaxation of isolated adult rat cardiomyocytes. In isolated perfused rat hearts, the SERCA2a activator 1 enhances systolic and diastolic functions. has not independently confirmed the accuracy of these methods. They are for reference only.

SERCA2a activator 1 (Compound A; 30mg/kg; intravenous injection; male Wistar rats) treatment significantly enhances the diastolic function in anesthetized normal rats. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:

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Powder -20°C 3 years；4°C 2 years

[1]. Kaneko M, et al. A pyridone derivative activates SERCA2a by attenuating the inhibitory effect of phospholamban. Eur J Pharmacol. 2017 Nov 5;814:1-8.

In Vitro: DMSO : 62.5 mg/mL (113.29 mM; ultrasonic and warming and heat to 80°C)配制储备液