Edoxaban

Catalog No.S7280 Synonyms: DU-176b

Edoxaban Chemical Structure

Molecular Weight(MW): 738.27

Edoxaban is a selective factor Xa inhibitor with Ki of 0.561 nM, >10 000-fold selectivity over thrombin and FIXa, and is also an orally bioavailable anticoagulant drug.

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Biological Activity

Description Edoxaban is a selective factor Xa inhibitor with Ki of 0.561 nM, >10 000-fold selectivity over thrombin and FIXa, and is also an orally bioavailable anticoagulant drug.
Targets
Factor Xa [1]
(Cell-free assay)
0.561 nM(Ki)
In vitro

In human plasma, Edoxaban doubles prothrombin time and activates partial thromboplastin time at 0.256 and 0.508 μM, respectively. [1]

In vivo Oral administration of Edoxaban produces potent anti-Xa activity and high drug concentration in plasma in rats and monkeys. In vivo, Edoxaban dose-dependently inhibits thrombus formation in rat and rabbit thrombosis models. [1]

Protocol

Animal Research:[1]
+ Expand
  • Animal Models: Venous stasis thrombosis model in rats and rabbits
  • Formulation: 0.5% methylcellulose
  • Dosages: 0.3–3 mg/kg (Rabbit); 0.5–12.5 mg/kg (Rat)
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (135.45 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 738.27
Formula

C24H30ClN7O4S.C7H8O3S.H2O

CAS No. 1229194-11-9
Storage powder
Synonyms DU-176b

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02952599 Not yet recruiting Venous Thromboembolism Daiichi Sankyo Inc.|Quintiles, Inc.|A+ Inc. March 2017 --
NCT02951039 Not yet recruiting Atrial Fibrillation Daiichi Sankyo Inc.|Quintiles, Inc.|A+ Inc. March 2017 --
NCT02942576 Not yet recruiting Atrial Fibrillation Daiichi Sankyo Europe, GmbH|Daiichi Sankyo Inc. March 2017 Phase 3
NCT02943785 Not yet recruiting Atrial Fibrillation Daiichi Sankyo Inc.|Chiltern International Inc. February 2017 Phase 3
NCT02866175 Not yet recruiting Atrial Fibrillation Daiichi Sankyo Inc.|European Cardiovascular Research Institute|Kompetenznetz Vorhofflimmern e.V.|Chiltern International Inc. February 2017 Phase 3
NCT02964949 Not yet recruiting Atrial Fibrillation Daiichi Sankyo Inc.|Quintiles, Inc. January 2017 --

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Factor Xa Signaling Pathway Map

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