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Betrixaban maleate is a highly potent, selective, and orally efficacious factor Xa (fXa) inhibitor
| Molecular Weight | 567.98 |
| Formula | C27H26ClN5O7 |
| CAS Number | 936539-80-9 |
| Solubility (25°C) | DMSO 100 mg/mL Water 1 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.
| Related Factor Xa Products |
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| Garadacimab
Garadacimab (CSL312) is a first-in-class, fully human IgG4 monoclonal antibody targeting activated factor XII (FXIIa). Garadacimab has the potential for hereditary angioedema research. |
| Abelacimab
Abelacimab (MAA868) is a fully human IgG1 monoclonal antibody that binds with high affinity to the catalytic structural domain of FXI and locks it in the zymogen conformation, thereby preventing its activation by FXIIa or thrombin. Abelacimab can be used in thromboembolic disease studies. |
| Osocimab
Osocimab (BAY 1213790), an anti-FXIa antibody (Ki=2.4 nM; EC50=0.2 nM). FXI inhibition may reduce the risk of thrombosis. Osocimab inhibits thrombin generation, and prolongs activated partial thromboplastin time. Osocimab exhibits anticoagulant effects. |
| 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. |
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