PF-4191834

Names

[ Name ]:
PF-4191834

[Synonym ]:
unii-yx55dxp4t1

Biological Activity

[Description]:

PF-4191834 (PF-04191834) is an orally active, noniron chelating, and non-redox inhibitor of the 5-Lipoxygenase (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].

[Related Catalog]:

Research Areas >> Inflammation/Immunology

Signaling Pathways >> Metabolic Enzyme/Protease >> 5-Lipoxygenase

[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].

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₂H₂₃N₃O₂S

[ Molecular Weight ]:
393.50200

[ Exact Mass ]:
393.15100

[ PSA ]:
96.43000

[ LogP ]:
4.92150

PF-4191834

Names

Biological Activity

Chemical & Physical Properties

Related Compounds