BMS-262084 is a potent, selective and irreversible inhibitor of factor XIa, with an IC50 of 2.8 nM against human factor XIa. BMS-262084 also inhibits human tryptase (IC50=5 nM). BMS-262084 exhibits antithrombotic effects.
| Molecular Weight | 425.48 |
| Formula | C18H31N7O5 |
| CAS Number | 253174-92-4 |
| Form | Solid |
| Solubility (25°C) | DMSO 50 mg/mL (ultrasonic and warming and heat to 60°C) |
| 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 |
|---|
| MK-2060
MK-2060 is a monoclonal antibody with dual activity to inhibit coagulation factors XI and Xia, blocking both the activation of coagulation factor XI and the downstream activity of the activated protein. It can be used in studies related to end-stage renal disease (ESRD). |
| Xisomab 3G3
Xisomab 3G3 is a recombinant human-derived monoclonal antibody to coagulation factor XI (F11) that blocks factor XI activation mediated by factor XIIa in a concentration-dependent manner. |
| FXIa-IN-13
FXIa-IN-13 is an Factor Xa inhibitor with antithrombotic activity. |
| EMD 495235
EMD 495235 is a potent and orally active coagulation factor Xa inhibitor with an IC50 of 5.5 nM and a Ki of 6.8 nM. |
| Frunexian
Frunexian (EP-7041) is a selective and potent inhibitor of coagulation factor XI/activated factor XI, targeting to factor XIa. |
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