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Edoxaban Tosylate Monohydrate

Cat. No. M2661
Edoxaban Tosylate Monohydrate Structure
Synonym:

DU-176b

Size Price Availability Quantity
5mg USD 75  USD75 In stock
10mg USD 115  USD115 In stock
50mg USD 420  USD420 In stock
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Quality Control
Biological Activity

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.

Customer Product Validations & Biological Datas
Source Thromb Res (2015). Figure 2. Edoxaban
Method Calibrated automated thrombogram assays
Cell Lines pooled citrated platelet-poor plasma
Concentrations 25 to 250 ng/mL
Incubation Time 15 min
Results A direct linear correlation was observed between plasma concentrations of edoxaban and the blood coagulation parameters PT ratio and INR across all thromboplastin reagents
Source Thromb Res (2015). Figure 1. Edoxaban
Method Thrombin generation test
Cell Lines pooled citrated platelet-poor plasma
Concentrations 0.02-3.65 μM
Incubation Time 15 min
Results Accordingly, the values of distributions of peak thrombin over time were significantly different between edoxaban and fondaparinux at the tested molar concentration (0.9 μM)
Protocol
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
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)
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.

Chemical Information
Molecular Weight 738.27
Formula C24H30ClN7O4S.C7H8O3S.H2O
CAS Number 1229194-11-9
Purity >98%
Solubility DMSO 90 mg/mL
Storage at -20°C
References

[1] Bounameaux H, et al. Drugs. Edoxaban: an update on the new oral direct factor Xa inhibitor.

[2] Mikkaichi T, et al. Drug Metab Dispos. Edoxaban transport via P-glycoprotein is a key factor for the drug's disposition.

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Keywords: Edoxaban Tosylate Monohydrate, DU-176b supplier, Factor Xa, inhibitors

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