TABLE 1

Inhibition of ATX-mediated hydrolysis of different LPC species

ATX inhibition by the selected compounds was assessed via Amplex Red choline release assay. Fluorescence was read initially and after 2-hour incubation at 37°C at Ex/Em λ of 560/590 nm. Data (relative fluorescence) were then recorded as a mean value of the triplicates for each sample and reported as % inhibition of ATX-mediated LPC hydrolysis.

% Inhibition (± S.D.)
CompoundLPC 14:0LPC 16:0LPC 18:0LPC 18:1
918013 (Compound 1)41.0 ± 5.155.4 ± 1.743.6 ± 2.651.8 ± 2.4
931126 (Compound 2)55.9 ± 0.569.0 ± 1.257.6 ± 0.961.9 ± 2.0
966791 (Compound 3)70.3 ± 1.880.3 ± 1.078.2 ± 1.178.8 ± 0.7