Free shipping on all orders over $ 500
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.
 |
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) |
| 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. |
| 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.
| Related Factor Xa Products |
|---|
| Milvexian
Milvexian (BMS-986177) is an orally bioavailable, reversible, direct inhibitor of human and rabbit factor (FXIa) with Ki values of 0.11 nM and 0.38 nM, respectively. |
| Asundexian
Asundexian (BAY2433334) is a reversible inhibitor of the active site of Factor XIa. Asundexian inhibits the activity of FXIa by directly, efficiently, and reversibly binding to its active site. the IC50 of human FXIa in Asundexian inhibition buffer is 1 nM. |
| Betrixaban maleate
Betrixaban maleate is a highly potent, selective, and orally efficacious factor Xa (fXa) inhibitor |
| Edoxaban tosylate
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
Edoxaban (DU-176) 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. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.
