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Table 1 In vitro activity of AVX001, AVX002, and DHA in the mixed micelle cPLA2α enzyme assay

From: Cytosolic group IVA phospholipase A2 inhibitors, AVX001 and AVX002, ameliorate collagen-induced arthritis

Name Structure In vitro enzyme activity
GIVA cPLA2 GVIA iPLA2 GV sPLA2 GIVA cPLA2
vesicle assay
% Inhibita XI(50) % Inhibita % Inhibita IC50 (nM)b
AVX001 90 0.0072 ± 0.0007 68 62 120 ± 58
AVX002 93 0.0057 ± 0.001 88 68 126 ± 37
DHA 8.9 ND 38 32 ND
  1. DHA Docosahexaenic acid, cPLA cytosolic phospholipase A2 protein, IC50 half maximal inhibitory concentration, ND not determined
  2. aMixed micelle enzyme in vitro assay: % inhibition at a 0.091 mol fraction of each inhibitor
  3. bVesicle enzyme in vitro data included for reference. Inhibitors were tested in the 0–3 μM range [11]