Specificity of Ixolaris to FVIIa/TF-induced FX activation
| Enzymes/substrates . | Residual activity (%) . |
|---|---|
| VIIa/TF (6.4 pM)/S2288 (1 mM) | 0 |
| Thrombin (125 pM)/S2238 (250 μM) | 103 ± 1.56 |
| Chymotrypsin (22.4 nM)/S2222 (250 μM) | 101.5 ± 0.09 |
| FXIa (58.7 pM)/S2256 (250 μM) | 89.2 ± 3.1 |
| Reptilase (0.3125 BU/mL)/S2238 (250 μM) | 98.5 ± 0.52 |
| Plasmin (5 mU/mL)/S2251 (250 μM) | 107.5 ± 0.75 |
| Elastase (250 pM)/substrate (500 μM) | 106 ± 8.02 |
| Tryptase (0.4 μg/mL)/S2222 (250 μM) | 101 ± 0.07 |
| Enzymes/substrates . | Residual activity (%) . |
|---|---|
| VIIa/TF (6.4 pM)/S2288 (1 mM) | 0 |
| Thrombin (125 pM)/S2238 (250 μM) | 103 ± 1.56 |
| Chymotrypsin (22.4 nM)/S2222 (250 μM) | 101.5 ± 0.09 |
| FXIa (58.7 pM)/S2256 (250 μM) | 89.2 ± 3.1 |
| Reptilase (0.3125 BU/mL)/S2238 (250 μM) | 98.5 ± 0.52 |
| Plasmin (5 mU/mL)/S2251 (250 μM) | 107.5 ± 0.75 |
| Elastase (250 pM)/substrate (500 μM) | 106 ± 8.02 |
| Tryptase (0.4 μg/mL)/S2222 (250 μM) | 101 ± 0.07 |
Ixolaris (32 nM, final concentration) was preincubated for 15 minutes at 37°C with the enzymes listed, followed by addition of the appropriate chromogenic substrate. Reactions were followed for 30 minutes at 37°C, and the effect of Ixolaris was estimated by setting the initial velocity obtained in the presence of enzyme alone (without inhibitor) as 100%.