1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. Calcium Channel
  3. SERCA2a activator 1

SERCA2a activator 1 

Cat. No.: HY-124873
Handling Instructions

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.

For research use only. We do not sell to patients.

SERCA2a activator 1 Chemical Structure

SERCA2a activator 1 Chemical Structure

CAS No. : 2139330-34-8

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Description

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].

IC50 & Target

SERCA2a[1]

In Vitro

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].

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.
Molecular Weight

551.66

Formula

C₃₂H₂₉N₃O₄S

CAS No.

2139330-34-8

SMILES

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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Keywords:

SERCA2a activator 1Calcium ChannelCa2+ channelsCa channelsSERCA2aCa2+phospholambansystolicdiastolicsarcoplasmicreticulumheartfailureInhibitorinhibitorinhibit

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SERCA2a activator 1
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