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Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
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
| Sonrisas canónicas | O=C(C1=CC(C(C=C2CC3=CC=CC=C3)=CN(CCCC)C2=O)=NC=C1)NS(=O)(C4=CC=C5C=CC=CC5=C4)=O |
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| Peso molecular | 551.66 |
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View spec sheet →| Solubilidad | DMSO : 62.5 mg/mL (113.29 mM; ultrasonic and warming and heat to 80°C) |
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