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Cat. No. M29698
BMS-262084  Structure
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Biological Activity

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.

Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
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.


[1] Pancras C Wong, et al. J Thromb Thrombolysis. A small-molecule factor XIa inhibitor produces antithrombotic efficacy with minimal bleeding time prolongation in rabbits

[2] Antonio Gómez-Outes, et al. Ther Adv Cardiovasc Dis. New parenteral anticoagulants in development

[3] William A Schumacher, et al. Eur J Pharmacol. Antithrombotic and hemostatic effects of a small molecule factor XIa inhibitor in rats

[4] Amrita V Kamath, et al. J Pharm Sci. Multiple pathways are involved in the oral absorption of BMS-262084, a tryptase inhibitor, in rats: role of paracellular transport, binding to trypsin, and P-glycoprotein efflux

[5] Xinhua Qian, et al. J Org Chem. A stereoselective synthesis of BMS-262084, an azetidinone-based tryptase inhibitor

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Keywords: BMS-262084  supplier, Factor Xa, inhibitors, activators

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