SERCA2a activator A

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

SERCA2a activator A 是一种新型肌/内质网 Ca2+ 依赖性 ATPase 2a (SERCA2a) 激活剂。

SERCA2a activator A is a novel sarco/endoplasmic reticulum Ca2+-dependent ATPase 2a (SERCA2a) activator that activates the Ca2+-dependent ATPase activity of cardiac SR vesicles but not that of skeletal muscle SR vesicles that lack of phospholamban (PLN); binds to PLN (Kd=75 uM), attenuates its inhibition of SERCA2a; enhances systolic and diastolic functions in rat hearts.

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. 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.

SERCA2a activator 1 (Compound A; 30mg/kg; intravenous injection; male Wistar rats) treatment significantly enhances the diastolic function in anesthetized normal rats. 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.

Compound A

GPCR/G Protein

Calcium Channel

Calcium Channel

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2139330-34-8

551.661

C32H29N3O4S

>98% (HPLC)

In Vitro:?DMSO : 62.5 mg/mL (113.29 mM)

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

5'-benzyl-1'-butyl-N-(naphthalen-2-ylsulfonyl)-6'-oxo-1',6'-dihydro-[2,3'-bipyridine]-4-carboxamide

(-20℃)

With Ice Pack

≥ 2 years