Product Overview
Factor Xa (FXa), a key serine protease, is a promising target enzyme for the prophylaxis and treatment of thromboembolic diseases. Edoxaban tosylate monohydrate is a novel antithrombotic agent that directly inhibits FXa activity. Clinical trial: A previous study determined the mass balance and pharmacokinetics of edoxaban in humans after oral administration of 14C edoxaban. The mass balance of edoxaban study showed unchanged edoxaban as the most abundant component. Edoxaban was eliminated through multiple pathways, but each accounts for only a small amount of overall elimination.
Molecular Formula
C31H40ClN7O8S2
Chemical Name
N-(5-chloropyridin-2-yl)-N-[(1S,2R,4S)-4-(dimethylcarbamoyl)-2-[(5-methyl-6,7-dihydro-4H-[1,3]thiazolo[5,4-c]pyridine-2-carbonyl)amino]cyclohexyl]oxamide; 4-methylbenzenesulfonic acid; hydrate
Solubility
Soluble in DMSO > 10 mM
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
In vitro
Edoxaban tosylate monohydrate (DU-176b) inhibited FXa with Ki values of 0.561 nM for free FXa, 2.98 nM for prothrombinase, and exhibited >10 000-fold selectivity for FXa. DU-176b doubled prothrombin time and activated partial thromboplastin time in human plasma. DU-176b did not impair platelet aggregation by ADP, collagen or U46619.
In vivo
DU-176b dose-dependently inhibited thrombus formation in rat and rabbit thrombosis models, although bleeding time in rats was not significantly prolonged at an antithrombotic dose.
Download Datasheet