Skip to main content
. 2019 Mar 20;10:263. doi: 10.3389/fphar.2019.00263

Table 3.

Inhibition of sEH by CysLT1RA.

sEH rec. sEH (HEP-G2) CysLT1R
IC50 [μM] [nM]
Zafirlukast 1.97 ± 0.08 μM 0.82 ± 0.24 μM 5
Montelukast n.d. 1.95 ± 0.30 μM 5
Pranlukast 8.86 ± 0.19 μM 14.11 ± 3.22 μM 4

sEH activities were determined with recombinant enzyme as well as HEP-G2 cell lysates. For determination of the activity of recombinant sEH, a fluorescence-based assay using PHOME as substrate was employed. In contrast, sEH activity in HEP-G2 cell lysates was measured by conversion of deuterated 14,15-EET into the corresponding diol by LC-MS/MS technique. Results are shown SEM of three independent experiments. n.d., not determined due to autofluorescence of the compound; rec, recombinant enzyme.