IC50 of NS 398, PD 137968, PD 138387 and indomethacin on isolated PGHS-1 or PGHS-2/ and RBL 5-LO
| Compound | oPGHS-1 | rhPGHS-2 | oPGHS-1/rhPGHS-2 | RBL 5-LO |
|---|---|---|---|---|
| NS-398 | NC100 μM (27% ± 4.0) | 0.19 ± 0.04 μM | >526 | NC100 μM (8.0% ± 0.6) |
| PD 137968 | NC30 μM (46% ± 14) | NC30 μM (43% ± 11.0) | NC | 3.5 μM* |
| PD 138387 | NC100 μM (7.5% ± 1.5) | 1.7 ± 0.70 μM | >58.9 | 14 μM* |
| Indomethacin | 0.012 ± 0.0006 μM | 5.9 ± 0.97 μM | 0.0020 | NC32 μM (0.75 ± 1.1) |
Average ± S.E. oPGHS-1 = ram seminal vesicles PGHS1; rhPGHS-2 = recombinant human PGHS-2; RBL-5LO = rat basophilic leukemia cell 5-LO. NC means inhibitory activity did not reach 50% inhibition, and IC50 or ratio could not be calculated. Values in parentheses represent the maximum inhibitory activity observed at the highest concentration used (indicated in the subscript). Solubility problems preventing testing of PD 137968 at higher concentration. * Single-run determination.