PF-4191834 (Synonyms: PF-04191834) |
| Catalog No.GC36883 |
PF-4191834 (PF-04191834) es un inhibidor no redox, quelante sin hierro y activo por vÍa oral de la 5-lipoxigenasa (5-LOX) (IC50 = 229 nM), muestra una selectividad de ~300 veces para 5-LOX durante 12 -LOX y 15-LOX, no muestra actividad hacia las enzimas ciclooxigenasas, y es eficaz en la inflamaciÓn y el dolor.
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Cas No.: 1029317-21-2
Sample solution is provided at 25 µL, 10mM.
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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]. IC50: 229 nM (5-LOX), 130 nM (human 5-LOX)[1]
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].
[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.
Average Rating: 5 (Based on Reviews and 35 reference(s) in Google Scholar.)
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