Pimobendan - 半岛电竞官方网址

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

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 vitroactivity: 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.

In Vitro

In vitroactivity: 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.

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