Edoxaban-d is intended for use as an internal standard for the quantification of edoxaban by GC- or LC-MS. Edoxaban is an orally bioavailable and potent inhibitor of factor Xa (Ks = 0.561 and 0.903 nM for free and complexed human factor Xa, respectively). It is >10,000-fold selective for factor Xa over thrombin, FVIIa/sTF, FXIa, tPA, aPC, trypsin, plasmin, and chymotrypsin. Edoxaban prolongs prothrombin, activated partial thromboplastin, and thrombin clotting times in a concentration-dependent manner ex vivo in human plasma. Oral administration of edoxaban (0.5-12.5 mg/kg) reduces thrombus formation and prolongs prothrombin time in a dose-dependent manner in rat and rabbit models of venous stasis thrombosis. It also reduces thrombus formation in a rat model of platinum wire-induced venous thrombosis. Formulations containing edoxaban have been used to prevent stroke in patients with atrial fibrillation.
Edoxaban-d6 is deuterium labeled Edoxaban. Edoxaban (DU-176) is a selective, potent and orally active factor Xa (FXa) inhibitor with Kis of 0.561 nM and 2.98 nM for free FXa and prothrombinase, respectively. Edoxaban is an anticoagulant agent and can be used for stroke prevention. Edoxaban is also a weak inhibitor of thrombin and factor IXaβ (FIXa), with Kis of 6.00 μM and 41.7 μM, respectively, exhibits >10000-fold selectivity for FXa. Edoxaban has antithrombotic properties and has potential for thromboembolic diseases treatment.
分子式
C24H24ClD6N7O4S
分子量
554.09484
CAS号
1304701-57-2
中文名称
依度沙班-d6;伊多塞班-d6;艾多沙班-d6
运输条件
Room temperature in continental US; may vary elsewhere.