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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Incubation time |
Animal Experiment | |
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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. |
Molecular Weight | 738.27 |
Formula | C24H30ClN7O4S.C7H8O3S.H2O |
CAS Number | 1229194-11-9 |
Solubility (25°C) | DMSO 90 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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.
[1] Bounameaux H, et al. Drugs. Edoxaban: an update on the new oral direct factor Xa inhibitor.
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