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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.
| 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 |
|---|
| Apixaban
Apixaban is a highly selective, reversible and orally active direct factor Xa inhibitor with an IC50 of 0.22±0.02 µM. |
| Rivaroxaban
Rivaroxaban (Xarelto, BAY 59-7939) is oral direct factor Xa inhibitor with an IC50 value of 2.1nM. |
| Edoxaban Tosylate Monohydrate
Edoxaban tosylate monohydrate is a selective factor Xa inhibitor with Ki of 0.561 nM, >10000-fold selectivity over thrombin and FIXa, and is also an orally bioavailable anticoagulant compound. |
| BMS-740808
BMS-740808 is a highly potent, selective inhibitor of blood coagulation factor Xa (fXa) with Ki with 0.03 nM. |
| Ozagrel
Ozagrel is a potent and selective thromboxane A2 synthetase inhibitor with an IC50 of 4 nM. |
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