Table 1

Inhibition kinetics of FXa or prothrombinase

Inhibitor
Antithrombin III, k2 ± SD × 103, M−1 s−1TFPI, Ki*, nM
Free FXa   
    wt-FXa 1.28 ± 0.060 0.07 ± 0.012 
    FXaI16L 0.03 ± 0.006 1.86 ± 0.340 
    FXaV17A 0.05 ± 0.002 1.16 ± 0.120 
Prothrombinase   
    wt-FXa 0.18 ± 0.010 ND 
    FXaI16L 0.09 ± 0.006 ND 
    FXaV17A 0.05 ± 0.003 ND 
Inhibitor
Antithrombin III, k2 ± SD × 103, M−1 s−1TFPI, Ki*, nM
Free FXa   
    wt-FXa 1.28 ± 0.060 0.07 ± 0.012 
    FXaI16L 0.03 ± 0.006 1.86 ± 0.340 
    FXaV17A 0.05 ± 0.002 1.16 ± 0.120 
Prothrombinase   
    wt-FXa 0.18 ± 0.010 ND 
    FXaI16L 0.09 ± 0.006 ND 
    FXaV17A 0.05 ± 0.003 ND 

The errors in the fitted constants represent ± 2 SDs. The data are representative of 2-3 independent measurements. Inhibition kinetics of FXa alone or prothrombinase were determined from initial velocity studies conducted with peptidyl substrate, Spec Xa. Details of the experimental design can be found in “Methods.”

ND, not determined.

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