product name Pimobendan
Description: Pimobendan is a potent and selective inhibitor of PDE3 with IC50 of 0.32 μM. Pimobendan is a veterinary medication. Pimobendan is both a calcium sensitizer and a selective inhibitor of phosphodiesterase III (PDE3) with positive inotropic and vasodilator effects. Pimobendan is used in the management of heart failure in dogs, most commonly caused by myxomatous mitral valve disease, or dilated cardiomyopathy.
References: J Cardiovasc Pharmacol. 1991 Jul;18(1):17-27; J Am Coll Cardiol. 1999 Apr;33(5):1400-7.
334.37
Formula
C19H18N4O2
CAS No.
74150-27-9
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
Synonyms
UD-CG-115
other peoduct :
| 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: Cell Assay: |
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| In Vivo | Pimobendan 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 model | Male DBA/2 mice of viral myocarditis |
| Formulation & Dosage | Suspended in 0.25% methylcellulose solution, in concentrations of 120 μg/mL and 12 μg/mL; 0.1 or 1 mg/kg; oral gavage |
| References | J Cardiovasc Pharmacol. 1991 Jul;18(1):17-27; J Am Coll Cardiol. 1999 Apr;33(5):1400-7. |
