Catalog No.S7280

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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Edoxaban Chemical Structure

Edoxaban Chemical Structure
Molecular Weight: 738.27

Validation & Quality Control

Quality Control & MSDS

Related Compound Libraries

Edoxaban is available in the following compound libraries:

Product Information

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Product Description

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]
IC50 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(Only for Reference)

Kinase Assay: [1]

Anti-FXa activity of Edoxaban FXa is added to the mixture of Edoxaban or 5% DMSO control and a chromogenic substrate S-2222 (250–1000 μM) in a reaction buffer (20 mm Tris–HCl, pH 7.4, 150 mm NaCl, 0.1% BSA). The final concentrations of FXa are as follows: human FXa (0.005 U/mL, 0.7 nM), rabbit FXa (0.005 U/mL, molarity unavailable), rat FXa (0.025 U/mL, 10 nM) and cynomolgus monkey FXa (0.025 U/mL, 3 nM). To measure amidolysis of S-2222 by FXa, the absorbance at 405 nm is monitored with a microplate spectrophotometer SPECTRAmax 340 at 30 °C for 10 min and the reaction velocity (mO.D./min) is obtained. The inhibition constant (Ki) values of Edoxaban are calculated by the Lineweaver–Burk plots and subsequent secondary plots.

Animal Study: [1]

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)


[1] Furugohri T, et al. J Thromb Haemost. 2008, 6(9), 1542-1549.

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-30)

NCT Number Recruitment Conditions Sponsor
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 Outcome  ...more 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,  ...more German Atrial Fibrillation Network|Daiichi Sankyo Europe, GmbH|Deutsches Zentrum für Herz-Kreislauf-Forschung February 2016 Phase 3

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Chemical Information

Download Edoxaban SDF
Molecular Weight (MW) 738.27


CAS No. 1229194-11-9
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms DU-176b
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 Name Ethanediamide, N1-(5-chloro-2-pyridinyl)-N2-[(1S,2R,4S)-4-[(dimethylamino)carbonyl]-2-[[(4,5,6,7-tetrahydro-5-methylthiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]cyclohexyl]-, 4-methylbenzenesulfonate, hydrate

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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