Name | Pimobendan |
Description | Pimobendan (UD-CG 115 BS) is a selective inhibitor of PDE3 (IC50: 0.32 μM). |
In vitro | Compared to the control group, Pimobendan (1 mg/kg) significantly reduced the permeability of cardiomyocytes and also decreased the levels of TNF-α and IL-1β within the chamber without affecting myocardial nerves, heart weight, and body weight. In a mouse model of EMC virus-induced myocarditis, Pimobendan contributed to an extension of lifespan. The final survival rate was significantly increased from 33.6% (control group) to 53.3% (0.1 mg/kg) or 66.7% (1 mg/kg). Additionally, Pimobendan inhibited the expression of inducible nitric oxide synthase genes in the heart, thereby reducing the content of nitric oxide within the heart. |
In vivo | When administered to human atrial cells, Pimobendan (100 μM) increased the L-type calcium current by 250.4% (EC50: 1.13 μM). Its effect on rabbit atrial cells was significantly lower, resulting in a 67.4% increase in ICa(L). Pimobendan exhibits selective inhibitory action on isolated PDE III in guinea pig myocardium (IC50: 0.32 μM), with much higher IC50s for PDE I and PDE II (>30 μM). It also inhibits cAMP-PDE III activity (IC50: 2.4 μM) and induces a positive inotropic effect on isolated guinea pig papillary muscles (EC50: 6.0 μM), partially due to its selective inhibition of myocardial PDE III. |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO : 55 mg/mL (164.49 mM) Ethanol : 5 mg/mL (14.95 mM) H2O : < 1 mg/mL (insoluble or slightly soluble)
|
Keywords | inhibit | Pimobendan | UD-CG-115 | UD-CG 115 | Phosphodiesterase (PDE) | Inhibitor |
Inhibitors Related | Theophylline monohydrate | Roflumilast | Theobromine | Apremilast | Isoprenaline hydrochloride | Indomethacin | Icariin | Theophylline | Vardenafil hydrochloride | Doxofylline |
Related Compound Libraries | Highly Selective Inhibitor Library | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | Anti-Neurodegenerative Disease Compound Library | EMA Approved Drug Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Cardiovascular Disease Compound Library | Metabolism Compound Library | Bioactive Compounds Library Max |