Table 7.
Potency of various inhibitors for carboxylesterases and selected serine hydrolases. Inhibitor potencies (IC50) were measured at 37°C in phosphate buffer (100 mM, pH = 8, 0.1 mg/mL BSA) containing ≤2% DMSO using either CMNA (hCE1, hCE2, hCE3, AADAC, PON1) or 1b (FAAH) as the substrate ([S]final= 50 µM). Values represent the average of triplicates for a single experiment.
| IC50 (µM) | |||
|---|---|---|---|
|
|
|||
| 2-chloro-3’,4’- dimethoxybenzil |
Loperamide | Thyroxine | |
|
|
|
|
|
| hCE1 | 2.5 | >100 | 1.5 |
| hCE2 | 0.014 | 0.65 | 16 |
| hCE3 | >100 | >100 | 23 |
| AADAC | >100 | 23 | 0.73 |
| FAAH | 7.6 | >100 | >100 |
| PON1 | 25 | >100 | 2.1 |
| Selectivity hCE2/hCE1 | 180 | >150 | 0.094 |