Edoxaban

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]
Features

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)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
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

References

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

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-23)

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 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
Formula

C24H30ClN7O4S.C7H8O3S.H2O

CAS No. 1229194-11-9
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms DU-176b
Solubility (25°C) * In vitro DMSO 100 mg/mL (135.45 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
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

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