SERCA2a activator 1

• CAT Number: I017142
• CAS Number: 2139330-34-8
• Molecular Formula: C32H29N3O4S
• Molecular Weight: 551.66
• Purity: ≥95%
• Synonyms: 2-(5-benzyl-1-butyl-6-oxopyridin-3-yl)-N-naphthalen-2-ylsulfonylpyridine-4-carboxamide
• InChI: InChI=1S/C32H29N3O4S/c1-2-3-17-35-22-28(19-27(32(35)37)18-23-9-5-4-6-10-23)30-21-26(15-16-33-30)31(36)34-40(38,39)29-14-13-24-11-7-8-12-25(24)20-29/h4-16,19-22H,2-3,17-18H2,1H3,(H,34,36)
• InChIKey: DBGJRQXKIIMWLS-UHFFFAOYSA-N
• SMILES: CCCCN1C=C(C=C(C1=O)CC2=CC=CC=C2)C3=NC=CC(=C3)C(=O)NS(=O)(=O)C4=CC5=CC=CC=C5C=C4

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].

Reference

[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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