Home Metabolism PDE inhibitor Pimobendan For research use only.

Pimobendan

Synonyms: UD-CG 115 BS

Pimobendan (UD-CG 115 BS) is a selective inhibitor of PDE3 with IC50 of 0.32 μM.

Pimobendan Chemical Structure

Pimobendan Chemical Structure

CAS: 74150-27-9

Selleck's Pimobendan has been cited by 3 publications

Purity & Quality Control

Batch: S155001 DMSO] 67 mg/mL] false] Ethanol] 5 mg/mL] false] Water] Insoluble] false Purity: 99.92%
99.92

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Biological Activity

Description Pimobendan (UD-CG 115 BS) is a selective inhibitor of PDE3 with IC50 of 0.32 μM.
Targets
PDE3 [1]
0.32 μM
In vitro
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
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]
Animal Research Animal Models Male DBA/2 mice of viral myocarditis
Dosages 0.1 or 1 mg/kg
Administration Orally once daily

Chemical lnformation & Solubility

Molecular Weight 334.37 Formula

C19H18N4O2
CAS No. 74150-27-9 SDF Download Pimobendan SDF
Smiles CC1CC(=O)NN=C1C2=CC3=C(C=C2)N=C(N3)C4=CC=C(C=C4)OC
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 67 mg/mL ( (200.37 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 5 mg/mL

Water : Insoluble


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In vivo
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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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