Pimobendan

Catalog No.S1550 Synonyms: UD-CG 115 BS

Pimobendan Chemical Structure

Molecular Weight(MW): 334.37

Pimobendan is a selective inhibitor of PDE3 with IC50 of 0.32 μM.

Size Price Stock Quantity  
In DMSO USD 230 In stock
USD 170 In stock
USD 320 In stock
USD 970 In stock
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Biological Activity

Description Pimobendan is a selective inhibitor of PDE3 with IC50 of 0.32 μM.
Targets
PDE3 [1]
0.32 μM
In vitro

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). [1] 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. [2] 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 [3]

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. [4]

Protocol

Animal Research:[4]
+ Expand
  • Animal Models: Male DBA/2 mice of viral myocarditis
  • Formulation: Prepared as an oral suspension in 0.25% methylcellulose solution, in concentrations of 120 μg/mL and 12 μg/mL
  • Dosages: 0.1 or 1 mg/kg
  • Administration: Orally once daily
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 67 mg/mL (200.37 mM)
Ethanol 5 mg/mL (14.95 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
0.5% methylcellulose
For best results, use promptly after mixing.
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 334.37
Formula

C19H18N4O2

CAS No. 74150-27-9
Storage powder
in solvent
Synonyms UD-CG 115 BS

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PDE Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID