Table 4.
Ki and IC50 values of PmDAP IV and human DPP IV for several gliptins.
| Classification | Compound | PmDAP IV | Human DPP IV | ||
|---|---|---|---|---|---|
| Ki (µM) | IC50 (µM) | Ki (nM) | IC50 (nM) | ||
| Class1 | Vildagliptin | 3.07 ± 0.39# | 18.8 ± 2.4 | 2.18 ± 0.25 | 8.04 ± 0.91 |
| Saxagliptin | 1.85 ± 0.13 | 11.1 ± 0.8 | 0.907 ± 0.013 | 3.35 ± 0.05 | |
| Class2 | Linagliptin | 30.0 ± 1.16 | 184 ± 7 | 0.00981 ± 0.00037 | 0.0362 ± 0.0014 |
| Trelagliptin | ND* | ND* | 0.340 ± 0.006 | 1.26 ± 0.02 | |
| Class3 | Sitagliptin | 4.00 ± 0.59 | 24.6 ± 3.6 | 3.31 ± 0.22 | 12.2 ± 0.8 |
| Teneligliptin | 2.34 ± 0.09 | 14. 3 ± 0.5 | 0.461 ± 0.004 | 1.70 ± 0.02 | |
| Anagliptin | 3.99 ± 0.07 | 24.5 ± 0.4 | 10.5 ± 0.6 | 38.6 ± 2.2 | |
| Omarigliptin | 23.8 ± 3.8 | 146 ± 23 | 0.520 ± 0.005 | 1.92 ± 0.02 | |
#Standard deviation obtained from three independent experiments. *Not determined due to a low inhibition rate (<30% using 100 µM of the compound).