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.
Product information
CAS Number: 2139330-34-8
Molecular Weight: 551.66
Formula: C32H29N3O4S
Chemical Name: 5'-benzyl-1'-butyl-N-(naphthalene-2-sulfonyl)-6'-oxo-1',6'-dihydro-[2,3'-bipyridine]-4-carboxamide
Smiles: CCCCN1C=C(C=C(CC2C=CC=CC=2)C1=O)C1=CC(=CC=N1)C(=O)NS(=O)(=O)C1=CC2=CC=CC=C2C=C1
InChiKey: DBGJRQXKIIMWLS-UHFFFAOYSA-N
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)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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. 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.
In Vivo:
SERCA2a activator 1 (Compound A; 30mg/kg; intravenous injection; male Wistar rats) treatment significantly enhances the diastolic function in anesthetized normal rats.
Products are for research use only. Not for human use.
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