A PDE3 inhibitor and ERG1 channel blocker (IC50s = 10.7

Vesnarinone – 1 mg

Brand:
Cayman
CAS:
81840-15-5
Storage:
-20
UN-No:
Non-Hazardous - /

Vesnarinone is an inhibitor of phosphodiesterase 3 (PDE3; IC50s = 10.7 and 13.2 μM for PDE3A and PDE3B, respectively).{41200} It also inhibits ether-a-go-go-related gene 1 (ERG1) channels (IC50 = 1.1 μM in HEK293T cells expressing human ERG1).{41201} Vesnarinone (3-300 μM) increases contractile tension in isolated ventricular muscles of dog, cat, rabbit, and guinea pig in a dose-dependent manner.{41202} Oral and i.v. administration of vesnarinone increases right ventricular pressure with no effect on heart rate in dog models of tricuspid insufficiency- and pulmonary stenosis-induced congestive heart failure. It also increases contractility and coronary flow while decreasing heart rate in a guinea pig model of aortic stenosis-induced congestive heart failure. Formulations containing vesnarinone have been used for the treatment of congestive heart failure.{41203}  

 

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SKU: 23489 - 1 mg Category:

Description

A PDE3 inhibitor and ERG1 channel blocker (IC50s = 10.7, 13.2, and 1.1 μM for PDE3A, PDE3B, and ERG1, respectively); increases contractile tension in isolated ventricular muscles of dog, cat, rabbit, and guinea pig in a dose-dependent manner; increases right ventricular pressure with no effect on heart rate in dog models of tricuspid insufficiency- and pulmonary stenosis-induced congestive heart failure; increases contractility and coronary flow while decreasing heart rate in a guinea pig model of aortic stenosis-induced congestive heart failure

Formal name: 6-[4-(3,4-dimethoxybenzoyl)-1-piperazinyl]-3,4-dihydro-2(1H)-quinolinone

Synonyms:  OPC 8212

Molecular weight: 395.5

CAS: 81840-15-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Blockers||Product Type|Biochemicals|Small Molecule Inhibitors|Phosphodiesterases||Research Area|Cardiovascular System|Cardiovascular Diseases|Atherosclerosis||Research Area|Cardiovascular System|Cardiovascular Diseases|Heart Failure||Research Area|Cardiovascular System|Heart|Arrhythmia||Research Area|Cardiovascular System|Heart|Myocardial Contractility||Research Area|Cardiovascular System|Vasculature

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