| Customization: | Available |
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| CAS No.: | 74150-27-9 |
| Formula: | C19h18n4o2 |
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Pizomendan is a chemical used to treat mild, moderate, or severe congestive heart failure caused by atrioventricular valve insufficiency or cardiac hypertrophy in dogs.
Biological activity
Pimobendan(UD-CG115BS) is a selective inhibitor of phosphodiesterase III(PDEIII) with an IC50 of 0.32μM. The target TargetValuePDE30.32μM
In vitro study
Pimobendan selectively inhibited PDEIII isolated from guinea pig myocardium with an IC50 of 0.32µM, and inhibited PDEI and PDEII with IC50s>30 µm. Pimobendan inhibited cAMP-PDEIII activity with an IC50 of 2.4μM and produced positive inotropic effects on isolated guinea pig papillary muscles with an EC50 of 6.0μM, in part due to selective inhibition of myocardial PDEIII. The effect of 100μMpimobendan on human atrial cells significantly increased the L-type calcium current (ICa(L) by 250.4%, and the EC50 was 1.13μM. Pimobendan increased ICa(L) in rabbit atrial cells by 67.4%, which was significantly lower than that in human atrial cells.
In vivo study
Pimobendan acts on the myocarditis murine model induced by EMC virus and has beneficial effect in prolonging life. Pimobendan treatment significantly improved final survival, from 33.6%(control group) to 53.3%(0.1mg/kg) or 66.7%(1mg/kg). Compared with the control group, Pimobendan treated at a dose of 1mg/kg significantly reduced the penetration of cardiomyocytes and the levels of intracavity tumor necrosis factor (TNF-α) and interleukin-1β, and had no effect on myocardial nerve, heart weight and body weight. Pimobendan inhibited the expression of iNOS gene in the heart and caused the decrease of NO production in the heart.
use
A cardiotonic. It has strong positive muscle strength and strong vasodilation and platelet aggregation. For the treatment of chronic and acute heart failure.
Jinan Hong Kongda Chemical Co., Ltd. is a high-tech enterprise specializing in the production of chemical raw materials and advanced pharmaceutical intermediates integrating scientific research, production and sales. The headquarter is located in Jinan, the capital of Shandong Province with major pharmaceutical province in China which has strong resource advantages.
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