| Identification | Back Directory | [Name]
SERCA2a activator A | [CAS]
2139330-34-8 | [Synonyms]
SERCA2a activator A
SERCA2a activator 1
[2,3'-Bipyridine]-4-carboxamide, 1'-butyl-1',6'-dihydro-N-(2-naphthalenylsulfonyl)-6'-oxo-5'-(phenylmethyl)- | [Molecular Formula]
C32H29N3O4S | [MDL Number]
MFCD34469372 | [MOL File]
2139330-34-8.mol | [Molecular Weight]
551.66 |
| Hazard Information | Back Directory | [Uses]
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[1]. | [Biological Activity]
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[1].
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[1]. 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[1].
SERCA2a activator 1 (Compound A; 30mg/kg; intravenous injection; male Wistar rats) treatment significantly enhances the diastolic function in anesthetized normal rats[1]. | [in vivo]
SERCA2a activator 1 (Compound A; 30mg/kg; intravenous injection; male Wistar rats) treatment significantly enhances the diastolic function in anesthetized normal rats[1]. | Animal Model: | Male Wistar rats (7-8 weeks old)[1] | | Dosage: | 30mg/kg | | Administration: | Intravenous injection | | Result: | Significantly enhanced the diastolic function in anesthetized normal rats. |
| [References]
[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. |
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