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Selectivity and biochemical characteristics of VD2173 and ZFH7116.
| VD2173 (18) | ZFH7116 (31) | |
|---|---|---|
| Matriptase IC50 (nM) | 2.2 | 21 |
| Hepsin IC50 (nM) | 11 | 0.38 |
| HGFA IC50 (nM) | 8610 | 26 |
| Thrombin IC50 (nM) | 8140 | 9000 |
| Factor Xa IC50 (nM) | 2048 | 770 |
| Solubility pH = 7.4 (μM) | 11 | 200 |
| Mouse [Human] Plasma Stability (t1/2, min) | 222 [>289] | 184 [140] |
| Mouse [Human] Microsomal Stability (t1/2, min) | >145 [>145] | >145 |
| Mouse PPB (% Free) | 28.6 | 16.7 |
