| CAS NO: | 74150-27-9 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| 1g | 电议 |
| 2g | 电议 |
| 5g | 电议 |
| Molecular Weight (MW) | 334.37 |
|---|---|
| Formula | C19H18N4O2 |
| 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 |
| Synonyms | UD-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 |
| 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 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. |
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