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Edoxaban tosylate

Cat. No. M14429
Edoxaban tosylate Structure
Synonym:

DU-176b

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Biological Activity

Edoxaban tosylate (DU-176b) 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 tosylate is an anticoagulant agent and can be used for stroke prevention. Edoxaban tosylate is a also weak inhibitor of thrombin and factor IXaβ (FIXa), with Kis of 6.00 μM and 41.7 μM, respectively, exhibits >10 000-fold selectivity for FXa. Edoxaban tosylate has antithrombotic properties and has potential for thromboembolic diseases treatment.

Chemical Information
Molecular Weight 720.26
CAS Number 480449-71-6
Solubility (25°C) DMSO 90 mg/mL
Storage 2-8°C, dry, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Gary E Raskob, et al. Edoxaban for the Treatment of Cancer-Associated Venous Thromboembolism

[2] Eri Toda Kato, et al. Efficacy and Safety of Edoxaban in Elderly Patients With Atrial Fibrillation in the ENGAGE AF-TIMI 48 Trial

[3] A T Cohen, et al. Comparison of the Novel Oral Anticoagulants Apixaban, Dabigatran, Edoxaban, and Rivaroxaban in the Initial and Long-Term Treatment and Prevention of Venous Thromboembolism: Systematic Review and Network Meta-Analysis

[4] Daniel A Hussar, et al. Edoxaban tosylate monohydrate, secukinumab, and suvorexant

[5] No authors listed. Edoxaban tosylate

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Keywords: Edoxaban tosylate, DU-176b supplier, Factor Xa, inhibitors, activators

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