Vesnarinone HCl

SKU: orb1745237

Description

Vesnarinone HCl (OPC-8212 HCl) is an oral PDE3 inhibitor that increases myocardial contractility by modulating calcium and potassium ion fluxes. This positive inotropic agent is used in research models of heart failure, including in vitro studies of cardiomyocyte function and in vivo hemodynamic assessments.

Research Area

Metabolism Research, Pharmacology & Drug Discovery

Key Properties

• MW: 431.91
• Purity: 95.72% (May vary between batches)
• Formula: C₂₂H₂₆ClN₃O₄
• SMILES: O=C(N1CCN(CC1)C2=CC=C3NC(CCC3=C2)=O)C4=CC=C(C(OC)=C4)OC.Cl
• Target: Potassium Channel,Calcium Channel,PDE

Bioactivity

• Target IC50:
  PDE3A:10.7 μM|ERG1:1.1 μM|PDE3B:13.2 μM
• In Vivo:
  Vesnarinone (3-300 μM) increases contractile tension in isolated ventricular muscles of dogs, cats, rabbits, and guinea pig in a dose-dependent manner. Vesnarinone (Oral and i.v.) administration of vesnarinone increases right ventricular pressure with no effect on heart rate in dog models of tricuspid insufficiency- and pulmonary stenosis-induced congestive heart failure. It also increases contractility and coronary flow while decreasing heart rate in a guinea pig model of aortic stenosis-induced congestive heart failure. Formulations containing vesnarinone have been used for the treatment of congestive heart failure.
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• In Vitro:
  Vesnarine (60 and 100 μg/mL; 48 h) in a dose-dependent manner to inhibit cell growth. Vesnarine (60 μg/mL; 48 h) induces G1 phase arrest and cell apoptosis. Vesnarine (60 μg/mL; 0, 12, 24, and 48 h) increased the expression of p21 mRNA and slightly decreased the p21 protein.
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Storage & Handling

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

Alternative Names

CalciumChannel, Ca(2+) receptor, Calcium Channel, PDE3, OPC-8212 HCl, Synonym 2, Synonym 2, Potassium Channel, PotassiumChannel, Vesnarinone HCl, Vesnarinone HCl(81840-15-5 Free base)

Compound Identifiers

PubChem CID

169553395