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    Pimobendan
    Pimobendan

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0782
    CAS #: 74150-27-9Purity ≥98%

    Description: Pimobendan (UD-CG115; UDCG115; Trade names Vetmedin, Acardi), a veterinary medication approved to treat CHF-congestive heart failure in dogs, is a potent and selective inhibitor of phosphodiesterase PDE3 with positive inotropic and vasodilator effects. It inhibits PDE3 with an IC50 of 0.32 μM. 

    References: J Cardiovasc Pharmacol. 1991 Jul;18(1):17-27; J Am Coll Cardiol. 1999 Apr;33(5):1400-7.

    Related CAS: 77469-98-8 (HCl); 118428-37-8 [(-)- Pimobendan]

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    Molecular Weight (MW)334.37
    FormulaC19H18N4O2
    CAS No.74150-27-9  (free base);
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 67 mg/mL (200.4 mM)
    Water:<1 mg/mL
    Ethanol: 5 mg/mL (14.95 mM)
    Solubility (In vivo)0.5% methylcellulose: 30mg/mL
    SynonymsUD-CG-115; UD-CG115; UD CG115; UD-CG 115; Pimobendan; pimobendane. Trade names: Vetmedin and Acardi 

    Chemical Name: 3-[2-(4-methoxyphenyl)-3H-benzimidazol-5-yl]-4-methyl-4,5-dihydro-1H-pyridazin-6-one

    InChi Key: GLBJJMFZWDBELO-UHFFFAOYSA-N

    InChi Code: InChI=1S/C19H18N4O2/c1-11-9-17(24)22-23-18(11)13-5-8-15-16(10-13)21-19(20-15)12-3-6-14(25-2)7-4-12/h3-8,10-11H,9H2,1-2H3,(H,20,21)(H,22,24)

    SMILES Code: O=C1CC(C)C(C2=CC=C3C(NC(C4=CC=C(OC)C=C4)=N3)=C2)=NN1


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    In Vitro

    In vitro activity: Pimobendan exhibits selective inhibition of PDE III isolated from guinea pig cardiac muscle with IC50 of 0.32 uM compared to the inhibition of PDE I and PDE II (IC50s >30 μM). Pimobendan inhibits the activity of cAMP-PDE III with IC50 of 2.4 μM. It also exerts concentration-dependent positive inotropic effects in isolated guinea-pig papillary muscles with a potency (EC50) of 6.0 μM, which is partly due to selective cardiac PDE III inhibition. In human atrial cells, 100 μM pimobendan significantly increases the L-type calcium current (ICa(L)) (evoked by depolarization to +10 mV from a holding potential of -40 mV) by 250.4% with the half-maximal stimulation (EC50) of 1.13 μM. In rabbit atrial cells, Pimobendan increases ICa(L) at +10 mV by 67.4.%, which is significantly lower than that obtained in human atrial cells.


    Kinase Assay: Pimobendan (UD-CG115) exhibits selective inhibition of PDE III isolated from guinea pig cardiac muscle with IC50 of 0.32 uM compared to the inhibition of PDE I and PDE II (IC50 >30 μM).


    Cell Assay: In human atrial cells, 100 μM Pimobendan (UD-CG115) significantly increases the L-type calcium current (ICa(L)) (evoked by depolarization to +10 mV from a holding potential of -40 mV) by 250.4% with the half-maximal stimulation (EC50 ) of 1.13 μM. In rabbit atrial cells, Pimobendan (UD-CG115) increases ICa(L) at +10 mV by 67.4.%, which is significantly lower than that obtained in human atrial cells.

    In VivoPimobendan shows a beneficial effect on survival in the murine model of EMC virus-induced myocarditis. Administration of Pimobendan significantly increases the final survival rate from 33.6% (control) to 53.3% (0.1 mg/kg) or 66.7% (1 mg/kg). Pimobendan (1 mg/kg) also significantly reduces myocardial cellular infiltration, the level of intracardiac tumor necrosis factor (TNF)-α and interleukin (IL)-1β compared with the control group, which shows no effect on myocardial necrosis, heart weight and body weight. Pimobendan suppresses expression of the intracardiac iNOS gene , causing reduction of intracardiac NO production.
    Animal modelMale DBA/2 mice of viral myocarditis
    Formulation & DosageSuspended in 0.25% methylcellulose solution, in concentrations of 120 μg/mL and 12 μg/mL; 0.1 or 1 mg/kg; oral gavage
    ReferencesJ Cardiovasc Pharmacol. 1991 Jul;18(1):17-27; J Am Coll Cardiol. 1999 Apr;33(5):1400-7.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Pimobendan

    Effect of pimobendan on survival rate after EMC virus inoculation.



    Pimobendan

    Typical histopathologic changes found seven days after EMC virus inoculation. J Am Coll Cardiol. 1999 Apr;33(5):1400-7.
     

    Pimobendan

    Effect of pimobendan on intracardiac NO production.



    Pimobendan

    Effect of pimobendan on intracardiac production of TNF-α, IL-1β, and IL-6 measured on day seven after EMC virus inoculation. J Am Coll Cardiol. 1999 Apr;33(5):1400-7.
     

    Pimobendan

    Quantification of iNOS mRNA in the hearts using RT-PCR. J Am Coll Cardiol. 1999 Apr;33(5):1400-7.
     


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