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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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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] Thrombin [1] FIXa [1]
0.561 nM(Ki) 6 μM(Ki) 41.7 μM(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
+ 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 <1 mg/mL
Ethanol <1 mg/mL
In vivo

* 1 mg/ml means slightly soluble or 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
in solvent
Synonyms DU-176b

Bio Calculators

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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02798471 Not yet recruiting Venous Thromboembolism|Pulmonary Embolism Daiichi Sankyo Inc. September 2016 Phase 3
NCT02801669 Not yet recruiting Atrial Fibrillation Daiichi Sankyo Co., Ltd.|Daiichi Sankyo Inc. June 2016 Phase 3
NCT02744092 Not yet recruiting Cancer|Venous Thromboembolism|Deep Vein Thrombosis (DVT)|Pulmonary Embolism (PE)|Blood Clot|VTE Alliance Foundation Trials, LLC.|Patient-Centered Outcomes Research Institute June 2016 --
NCT02567461 Recruiting Coronary Artery Disease University of Florida|Daiichi Sankyo Inc. March 2016 Phase 4
NCT02618577 Not yet recruiting Atrial High Rate Episodes German Atrial Fibrillation Network|Daiichi Sankyo Europe, GmbH|Deutsches Zentrum für Herz-Kreislauf-Forschung February 2016 Phase 3
NCT02611635 Recruiting Atrial Fibrillation Bayer February 2016 --

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Factor Xa Signaling Pathway Map

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