e4021

E4021 is a highly selective and potent small molecule inhibitor of type V phosphodiesterase (PDE5), and also an exceptionally potent inhibitor of PDE6[1][3][5]. Its primary mechanism is to inhibit phosphodiesterase-mediated hydrolysis of cyclic guanosine monophosphate (cGMP), leading to increased cGMP concentrations, which results in vasorelaxation and anti-platelet effects[1][5]. It has been investigated for its ability to inhibit platelet adhesion/aggregation, reduce pulmonary artery pressure (especially in equine veterinary trials as a potential Lasix alternative for exercise-induced pulmonary hemorrhage), and treat cardiovascular diseases[1][2][3]. In vitro studies show its competitive inhibition both on PDE5 and PDE6, with strong inhibitory binding at nanomolar concentrations[5]. Development was led by Eisai Co Ltd[3].

Other names

sodium 1-[6-chloro-4-(3,4-methylenedioxybenzyl)-aminoquinazolin-2-yl]piperidine-4-carboxylate sesquihydrate