Table 1.
Cmpd # |
Human sEH | Murine sEH | Microsomal Stability 1 | |
---|---|---|---|---|
Human | Mouse | |||
IC50 (nM) 2 | % Remaining at 1 h | |||
1 | 3.1 | 6.0 | 1.0 | 1.0 |
6a | 34.5 | 0.4 | 0.3 | 0.0 |
6b | 30.2 | 0.4 | 0.0 | 0.0 |
6c | 1.6 | 0.4 | 5.5 | 5.1 |
6d | 1.0 | 0.4 | 7.0 | 1.4 |
6e | 2.8 | 0.5 | 0.6 | 0.2 |
6f | 2.4 | 0.4 | 1.3 | 0.5 |
6g | 37.5 | 3.3 | 0.1 | 0.1 |
6h | 21.4 | 12.9 | 0.3 | 0.1 |
10a | 0.6 | 0.7 | 0.1 | 0.1 |
10b | 3.4 | 0.4 | 0.0 | 0.1 |
10c | 0.4 | 0.7 | 60 | 29 |
10d | 0.4 | 0.2 | 11 | 2 |
10e | 1.7 | 0.7 | 52 | 6 |
1 Percentage of remaining compound after 60 min of incubation with human and mouse microsomes obtained from Tebu-Xenotech in the presence of NADPH at 37 °C. See Materials and Methods for further details. The 2 IC50 values are the average of three replicates. The fluorescent assay as performed here has a standard error between 10 and 20% suggesting that differences of two-fold or greater are significant. Because of the limitations of the assay, it is difficult to distinguish among potencies < 0.5 nM [28].