PF-03049423

PF-03049423 is a potent and highly selective small molecule inhibitor of phosphodiesterase type 5A (PDE5A), with an IC50 in the sub-nanomolar range for rat and human platelet enzyme. It is orally active and brain penetrant. The drug was initially developed by Pfizer for potential use in acute ischemic stroke and as an antihypertensive agent due to its ability to enhance nitric oxide signaling pathways via inhibition of cGMP degradation, leading to vasodilation. Despite a satisfactory safety profile in clinical trials up to phase II for acute ischemic stroke, no therapeutic efficacy was demonstrated and development was discontinued[1][2][3][4][6][7].

Other names

3-[4-(2-hydroxyethyl)piperazin-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)-1H,2H-pyrido[3,4-b]pyrazin-2-oneCHEMBL591501CHEMBL-591501CHEMBL 591501954138-07-9