1029317-21-2

1029317-21-2 structure

Name: PF-4191834
Chemical Name: 4-[3-[4-(2-methylpyrazol-3-yl)phenyl]sulfanylphenyl]oxane-4-carboxamide
CAS Number: 1029317-21-2
Molecular Formula: C₂₂H₂₃N₃O₂S
Molecular Weight: 393.50200
Catalog: Signaling Pathways Metabolic Enzyme/Protease 5-Lipoxygenase
Create Date: 2016-03-29 11:45:48
Modify Date: 2024-01-11 14:15:47
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].

Name	4-[3-[4-(2-methylpyrazol-3-yl)phenyl]sulfanylphenyl]oxane-4-carboxamide
Synonyms	unii-yx55dxp4t1

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.