Vesnarinone (C007B-432829)

Vesnarinone (OPC-8212) is an orally active phosphodiesterase 3 ( PDE3 ) inhibitor. Vesnarinone can increase in calcium flux and decrease in potassium flux. Vesnarinone shows dose-dependent positive inotropic activity. Vesnarinone can be used in heart failure research.In VitroVesnarinone (60 and 100 μg/mL; 48 h) inhibits the cell growth in a dose-dependent manner. Vesnarinone (60 μg/mL; 48 h) induces G1 arrest and apoptosis. Vesnarinone (60 μg/mL; 0, 12, 24, and 48 h) treatment increases p21-mRNA expression and decreases p21 protein slightly. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: OSC3, OSC4, and OSC5 cells Concentration: 60 μg/mL and 100 μg/mL Incubation Time: 48 hours Result: Observed more than 50% inhibition in cells treated with 100 μg/mL, and reduced 30±40% the production of MTT formazan in cells treated with 60 μg/mL. Apoptosis AnalysisCell Line: OSC3, OSC4, and OSC5 cells Concentration: 60 μg/mL Incubation Time: 48 hours Result: Decreased the tumor cell population in the S phase and increased in the G1 phase. Western Blot AnalysisCell Line: OSC3, OSC4, and OSC5 cells Concentration: 60 μg/mL Incubation Time: 0, 12, 24, and 48 hours Result: Increased the expression of p21-mRNA after 12±24 h vesnarinone treatment. Decreased p21 protein slightly after 24 h treatment in OSC4.In VivoVesnarinone (oral gavage; 300 mg/kg; once daily; 6 w) binds covalently to rat liver in vivo. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female Lewis rats (200 g)Dosage: 300 mg/kg Administration: Oral gavage; 300 mg/kg; once daily; 6 weeks Result: Observed covalently modified liver proteins.Form:Solid. Specification: 0.98 Molecular Formula: C22H25N3O4 Molecular Weight: 395.45 PubChem CID: 5663 Isomeric SMILES: COC1=C(C=C(C=C1)C(=O)N2CCN(CC2)C3=CC4=C(C=C3)NC(=O)CC4)OC