A PDE3 inhibitor
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Enoximone

Item No. 30868

Technical Information
Formal Name
1,3-dihydro-4-methyl-5-[4-(methylthio)benzoyl]-2H-imidazol-2-one
CAS Number
77671-31-9
Synonyms
  • MDL 17043
Molecular Formula
C12H12N2O2S
Formula Weight
Purity
≥98%
Formulation
A solid
SMILES
CSC1=CC=C(C(C2=C(C)NC(N2)=O)=O)C=C1
InChi Code
InChI=1S/C12H12N2O2S/c1-7-10(14-12(16)13-7)11(15)8-3-5-9(17-2)6-4-8/h3-6H,1-2H3,(H2,13,14,16)
InChi Key
ZJKNESGOIKRXQY-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Enoximone is a phosphodiesterase 3 (PDE3) inhibitor (IC50 = 5.9 µM).1 It is selective for PDE3 over PDE1, -2, and -4 (IC50s = 2,100, 2,900, and 21.1 µM, respectively). Enoximone increases the force of contraction and cAMP levels in isolated canine right ventricular trabeculae, an effect that can be reversed by carbamoylcholine (carbachol; Item No. 14486).2 In vivo, enoximone (0.1-1 mg/kg) increases cardiac contractile force in dogs.3 Formulations containing enoximone have been used in the treatment of congestive heart failure.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Bethke, T., Eschenhagen, T., Klimkieqicz, A., et alPhosphodiesterase inhibition by enoximone in preparations from nonfailing and failing human hearts. Arzneimittelforschung 42(4), 437-445 (1992).

    2. Endoh, M., Yanagisawa, T., Morita, T., et alDifferential effects of sulmazole (AR-L 115 BS) on contractile force and cyclic AMP levels in canine ventricular muscle: Comparison with MDL 17,043. J. Pharmacol. Exp. Ther. 234(1), 267-273 (1985).

    3. Dage, R.C., Roebel, L.E., Hsieh, C.P., et alCardiovascular properties of a new cardiotonic agent: MDL 17,043 (1.3-dihydro-4-methyl-5-[4-(methylthio)-benzoyl]-2H-imidazol-2-one). J. Cardiovasc. Pharmacol. 4(3), 500-508 (1982).