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Betrixaban is a highly potent, selective, and orally efficacious factor Xa inhibitor with IC50 of 1.2 nM(inhibition of Factor 10a).Betrixaban is an oral direct inhibitor being developed for the prevention of venous thromboembolism (VTE).Betrixaban demonstrates antithrombotic activity and appeared well tolerated in knee replacement patients at the doses studied.
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Source | Expert Opin Pharmacother (2013). Figure 2. Betrixaban |
| Method | PK--PD analysis | |
| Cell Lines | ||
| Concentrations | 27.7 ng/mL and 58.6 ng/mL | |
| Incubation Time | 3.17 h | |
| Results | The median time of maximum plasma concentration (Tmax) for betrixaban occurred at 3.17 h after dosing for both dose groups |
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Source | Expert Opin Pharmacother (2013). Figure 1. Betrixaban |
| Method | PK--PD analysis | |
| Cell Lines | ||
| Concentrations | 27.7 ng/mL and 58.6 ng/mL | |
| Incubation Time | 3.17 h | |
| Results | The PK--PD modeling results demonstrated that betrixaban had no effect on cardiac repolarization |
| Cell Experiment | |
|---|---|
| Cell lines | whole blood |
| Preparation method | In a tissue factor-induced thrombin generation assay, betrixaban in concentrations ranging from 5 ng/mL to 25 ng/mL inhibited thrombin generation to a comparable degree as trough, and the peak levels were achieved by 2.5 mg fondaparinux. |
| Concentrations | 5 ng/mL to 25 ng/mL |
| Incubation time | 3–4 h |
| Animal Experiment | |
|---|---|
| Animal models | rabbit vena cava |
| Formulation | 0.5% methylcellulose |
| Dosages | 3 mg/kg |
| Administration | i.v. |
| 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.
| Molecular Weight | 451.91 |
| Formula | C23H22ClN5O3 |
| CAS Number | 330942-05-7 |
| Purity | >98% |
| Solubility | DMSO 10 mM |
| Storage | at -20°C |
| Related Factor Xa Products |
|---|
| Ozagrel sodium
Ozagrel(OKY-046) sodium salt is an antiplatelet agent working as a thromboxane A2 synthesis inhibitor. |
| Ozagrel
Ozagrel is a potent and selective thromboxane A2 synthetase inhibitor with an IC50 of 4 nM. |
| Edoxaban Tosylate Monohydrate
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 compound. |
| Rivaroxaban
Rivaroxaban (Xarelto, BAY 59-7939) is oral direct factor Xa inhibitor with an IC50 value of 2.1nM. |
| Apixaban
Apixaban is a highly selective, reversible and direct factor Xa inhibitor with an IC50 of 0.22±0.02 µM. |
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