Table A2.
Inhibitory profiles for the serine protease inhibitors UAMC‐00050, UAMC‐01162 and nafamostat mesilate
| Proteases | UAMC‐00050 | UAMC‐01162 | Nafamostat mesilate |
|---|---|---|---|
| IC50 (μM) | IC50 (μM) | Est. IC50 (μM) | |
| uPA | 0.0042 | 0.0031 | <0.001 |
| tPA | 7 | 23 | >2.5 |
| Plasmin | 0.9 | 13 | ±0.05 |
| Thrombin | 0.39 | 17 | ±0.5 |
| FXa | 100 | ±250 | ±2 |
| FXIIa | 1.61 | >2.5 | ±0.1 |
| Matriptase | 0.0025 | 0.083 | <0.001 |
| Tryptase | 0.028 | 0.093 | <0.001 |
| Cathepsin G | 0.12 | 0.33 | ±0.25 |
| HNE | >2.5 | >2.5 | >2.5 |
| Plasma KLK | >2.5 | >2.5 | ±0.005 |
| KLK1 | >2.5 | >2.5 | ±1 |
| KLK2 | 0.11 | 3 | ±0.1 |
| KLK4 | 0.0017 | 0.009 | ±0.005 |
| KLK8 | 0.0016 | 0.028 | ±0.015 |
| AChE | >20 | >10 | >2.5 |
Data are presented as mean. Est., estimated; FXa, factor Xa; FXIIa, factor XIIa; HNE, human neutrophil elastase; tPA, tissue plasminogen activator; uPA, urokinase plasminogen activator.