Uses
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].
Biological Activity
PF-4191834 (PF-04191834) is an orally active, non-iron-chelating, non-redox 5-lipoxygenase (5-LOX) inhibitor (IC50=229 nM), 5-LOX is about 300 times more selective than 12-LOX and 15-LOX, has no activity against cyclooxygenase, and is effective against inflammation and pain.
in vitro
PF-4191834 (PF-04191834) inhibits the synthesis of the 5-LOX products 5-HETE, 5-oxo-ETE, LTB4, and LTE4 with estimated IC 50 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. PF-4191834 (PF-04191834) exerts a concentration-dependent inhibition of human 5-LOX, with an IC 50 value of 130 nM and an IC 80 value of 370 nM.
References
[1] Masferrer JL, et al. Pharmacology of PF-4191834, a novel, selective non-redox 5-lipoxygenase inhibitor effective in inflammation and pain. J Pharmacol Exp Ther. 2010 Jul;334(1):294-301. DOI:
10.1124/jpet.110.166967
