|Description||Vesnarinone, a quinolinone derivative, is a cardiotonic agent. It has pharmacodynamic effects include inhibition of phosphodiesterase III (PDE3) activity, increases in calcium flux and decreases in potassium flux. Its IC50 value is 1 μM and 300 μM for inhibition of HERG channels and PDE. It is a novel cytokine inhibitor, for the treatment of lung fibrosis using a murine model of bleomycin (BLM)-induced pulmonary fibrosis. It is a new and novel inotropic drug that has unique and complex mechanisms of action. It inhibits phosphodiesterase, thereby leading to increased intracellular calcium, and also affects numerous myocardial ion channels, resulting in the prolongation of the opening time of sodium channels and the decrease in the delayed outward and inward rectifying potassium current. It plays an important role in the regulation of cytokines and suggests that the reduction of cytokine release may contribute to the beneficial effects of the drug in the treatment of heart failure. It inhibits the production of TFN-a and IFN-y by LPS stimulated whole blood from patients with heart failure and from healthy volunteers. It reduces the circulating levels of TNF-α in vivo. It improves ventricular performance most in patients with the worst degree of heart failure.|
|Synonyms||RG-0210; RG 0210; RG0210; OPC-8212; OPC 8212; OPC8212; Piteranometozine; Vesnarinone; Arkin; Arkin-Z. OPC 8212;6-[4-(3,4-Dimethoxybenzoyl)-1-piperazinyl]-3,4-dihydro-2(1H)-quinolinone;3,4-Dihydro-6-(4-(3,4-dimethoxybenzoyl)-1-piperazinyl)-2(1h)-quinolinone|
|Solubility||10 mM in DMSO|
|Application||Vesnarinone inhibits phosphodiesterase, thereby leading to increased intracellular calcium, and also affects numerous myocardial ion channels, resulting in the prolongation of the opening time of sodium channels and the decrease in the delayed outward and inward rectifying potassium current. It improves ventricular performance most in patients with the worst degree of heart failure.|
|Quality Standard||In-house standard|
|Shelf Life||2 month in rt, long time|
|Boiling Point||678.3±55.0 °C | Condition: Press: 760 Torr|
|Melting Point||238.1-239.8 °C|
|Density||1.246±0.06 g/cm3 | Condition: Temp: 20 °C Press: 760 Torr|
|Current Developer||Vesnarinone has been listed.|
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