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BMS-593214 

Cat. No. M27608
BMS-593214  Structure
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Quality Control & Documentation
Biological Activity

BMS-593214 is an active site-directed factor (F) VIIa inhibitor. BMS-593214 shows antithrombotic and antihaemostatic properties. BMS-593214 is a direct competitive inhibitor of human FVIIa and a non-competitive inhibitor of Viia-activated substrate FX. BMS-593214 prevents electroinduced carotid artery thrombosis (AT) and wire induced vena cava thrombosis (VT).

Chemical Information
Molecular Weight 505.56
Formula C31H27N3O4
CAS Number 1004551-40-9
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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.

References

[1] E Scott Priestley, et al. Bioorg Med Chem Lett. Discovery and gram-scale synthesis of BMS-593214, a potent, selective FVIIa inhibitor

[2] S Aditya. J Postgrad Med. Oral and parenteral anticoagulants: new kids on the block

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

[4] Pancras C Wong, et al. Thromb Haemost. Apixaban, a direct factor Xa inhibitor, inhibits tissue-factor induced human platelet aggregation in vitro: comparison with direct inhibitors of factor VIIa, XIa and thrombin

[5] Pancras C Wong, et al. Thromb Haemost. BMS-593214, an active site-directed factor VIIa inhibitor: enzyme kinetics, antithrombotic and antihaemostatic studies

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Keywords: BMS-593214  supplier, inhibitors, activators


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