SERCA2a activator A manufacturers
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| | SERCA2a activator A Basic information |
| Product Name: | SERCA2a activator A | | Synonyms: | SERCA2a activator A;[2,3'-Bipyridine]-4-carboxamide, 1'-butyl-1',6'-dihydro-N-(2-naphthalenylsulfonyl)-6'-oxo-5'-(phenylmethyl)-;SERCA2a activator 1;Ca channels,phospholamban,Inhibitor,Ca2+ channels,SERCA2a activator 1,SERCA2a,SERCA-2a activator 1,failure,reticulum,Calcium Channel,Ca2+,sarcoplasmic,diastolic,heart,systolic,inhibit;SERCA2a activator 1, 10 mM in DMSO;5'-Benzyl-1'-butyl-N-(naphthalen-2-ylsulfonyl)-6'-oxo-1',6'-dihydro-[2,3'-bipyridine]-4-carboxamide | | CAS: | 2139330-34-8 | | MF: | C32H29N3O4S | | MW: | 551.66 | | EINECS: | | | Product Categories: | | | Mol File: | 2139330-34-8.mol |  |
| | SERCA2a activator A Chemical Properties |
| storage temp. | Store at -20°C | | form | Solid | | color | Light yellow to yellow |
| | SERCA2a activator A Usage And Synthesis |
| 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. |
| | SERCA2a activator A Preparation Products And Raw materials |
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