Vesnarinone

SKU: orb1223044

Description

Vesnarinone is a cardiotonic agent, mixed phosphodiesterase 3 inhibitor and ion-channel modifier that has modest, dose-dependent, positive inotropic activity, but minimal negative chronotropic activity. Vesnarinone improves ventricular performance most in patients with the worst degree of heart failure.(In Vitro):Vesnarinone (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.(In Vivo):Vesnarinone (oral gavage; 300 mg/kg; once daily; 6 w) binds covalently to rat liver in vivo.

Key Properties

• CAS Number: 81840-15-5
• MW: 395.46
• Purity: >98% (HPLC)
• Formula: C₂₂H₂₅N₃O₄
• SMILES: N1C(=O)CCc2cc(ccc12)N1CCN(CC1)C(=O)c1cc(c(cc1)OC)OC
• Target: GSK-3
• Solubility: DMSO : 16.67 mg/mL. 42.15 mM

Bioactivity

• In Vivo:
  Vesnarinone (oral gavage; 300 mg/kg; once daily; 6 w) binds covalently to rat liver In vivo. 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.
• In Vitro:
  Vesnarinone (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. Cell Viability Assay Cell 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 Analysis Cell 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 analysis. Cell 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

RG-0210 | RG 0210 | Piteranometozine | Vesnarinone

Quick Database Links

Gene Symbol

GSK-3