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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. |
| Molecular Weight | 451.91 |
| Formula | C23H22ClN5O3 |
| CAS Number | 330942-05-7 |
| Solubility (25°C) | DMSO 10 mM |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Factor Xa Products |
|---|
| Darexaban
Darexaban (YM150) is a potent, selective and orally active factor Xa (FXa) inhibitor with an IC50 of 54.6 nM. |
| Eribaxaban
Eribaxaban (PD-0348292) is an orally active and selective FXa inhibitor with a Ki value of 0.32 nM. |
| Suc-Ile-Glu(γ-pip)-Gly-Arg-pNA hydrochloride
Suc-Ile-Glu(γ-pip)-Gly-Arg-pNA hydrochloride is a factor Xa specific chromogenic substrate. |
| D-Pro-Phe-Arg-Chloromethylketone
D-Pro-Phe-Arg-Chloromethylketone, a inhibitor of coagulation factor XII and plasma kallikrein, plays an important role in thrombosis and inflammation. |
| Methoxycarbonyl-D-Nle-Gly-Arg-pNA
Methoxycarbonyl-D-Nle-Gly-Arg-pNA is a synthetic trypsin that can serve as a substrate for coagulation factors IXa (FIXa) and Xa (FXa). |
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