A PDE3 inhibitor and ERG1 channel blocker
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Vesnarinone

Item No. 23489

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-[4-(3,4-dimethoxybenzoyl)-1-piperazinyl]-3,4-dihydro-2(1H)-quinolinone
CAS Number
81840-15-5
Synonyms
  • OPC 8212
Molecular Formula
C22H25N3O4
Formula Weight
395.5
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 3 mg/mlDMSO: 3 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml
λmax
272 nm
SMILES
COC1=CC=C(C(N2CCN(C3=CC(CCC(N4)=O)=C4C=C3)CC2)=O)C=C1OC
InChi Code
InChI=1S/C22H25N3O4/c1-28-19-7-3-16(14-20(19)29-2)22(27)25-11-9-24(10-12-25)17-5-6-18-15(13-17)4-8-21(26)23-18/h3,5-7,13-14H,4,8-12H2,1-2H3,(H,23,26)
InChi Key
ZVNYJIZDIRKMBF-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $153

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    10 mg

    $268

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    25 mg

    $587

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    Product Description

    Vesnarinone is an inhibitor of phosphodiesterase 3 (PDE3; IC50s = 10.7 and 13.2 μM for PDE3A and PDE3B, respectively).1 It also inhibits ether-a-go-go-related gene 1 (ERG1) channels (IC50 = 1.1 μM in HEK293T cells expressing human ERG1).2 Vesnarinone (3-300 μM) increases contractile tension in isolated ventricular muscles of dog, cat, rabbit, and guinea pig in a dose-dependent manner.3 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.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Nikpour, M., Sadeghian, H., Saberi, M.R., et al. Design, synthesis and biological evaluation of 6-(benzyloxy)-4-methylquinolin-2(1H)-one derivatives as PDE3 inhibitors. Bioorg. Med. Chem. 18(2), 855-862 (2010).

    2. Katayama, Y., Fujita, A., Ohe, T., et al. Inhibitory effects of vesnarinone on cloned cardiac delayed rectifier K+ channels expressed in a mammalian cell line. J. Pharmacol. Exp. Ther. 294(1), 339-346 (2000).

    3. Feldman, A.M. Pharmacologic properties and clinical evaluation of the new inotropic agent OPC-8212 (vesnarinone). Cardiovasc. Drug Rev. 11(1), 1-11 (1993).

    4. Reis, S.E., Holubkov, R., Young, J.B., et al. Estrogen is associated with improved survival in aging women with congestive heart failure: Analysis of the vesnarinone studies. J. Am. Coll. Cardiol. 36(2), 529-533 (2000).