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

Related Compounds

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.