PF-4191834 (PF-04191834) is an orally active, noniron chelating, and non-redox inhibitor of the 5-Lipoxygenase (5-LOX) (IC₅₀=229 nM), displays ~300-fold selectivity for 5-LOX over 12-LOX and 15-LOX, shows no activity toward the cyclooxygenase enzymes, and is effective in inflammation and pain^[1]. IC50 & Target: IC50: 229 nM (5-LOX), 130 nM (human 5-LOX)^[1] In Vitro: PF-4191834 (PF-04191834) inhibits the synthesis of the 5-LOX products 5-HETE, 5-oxo-ETE, LTB4, and LTE4 with estimated IC₅₀ values between 100 and 190 nM and do not inhibit significantly the COX-1/2 enzymes or the 12- or 15-LOX enzymes at concentrations up to 30 μM^[1].
PF-4191834 (PF-04191834) exerts a concentration-dependent inhibition of human 5-LOX, with an IC₅₀ value of 130 nM and an IC₈₀ value of 370 nM^[1].