AK106-001616 (AK 106-001616) is a potent and selective inhibitor of cytosolic phospholipase A2 (cPLA2) with IC50 of 3.8 nM (human cPLA2 enzyme).
AK106-001616 also inhibited rat cPLA2 with IC50 of 4.3 nM, shows no significant activity against human iPLA2, bovine sPLA2 IB and PAF-AH (>10,000 fold selectivity).
AK106-001616 suppressed the release of AA from Ca2+ ionophore A23187-stimulated rat RBL-2H3 cells (IC50=5.5 nM), also suppressed the production of PGE2 by LPS-stimulated human PBMCs (IC50=5.1 nM) and the production of LTB4 by Ca2+ ionophore A23187-stimulated RBL-2H3 cells (IC50=2.6 nM).
AK106-001616 demonstrates in vivo efficacy for inflammation, neuropathic pain, and pulmonary fibrosis.
