Cat. No. 1311
Alternative Name: L-663,536
Chemical Name: 1-[(4-Chlorophenyl)methyl]-3-[(1,1-
Biological ActivityAn inhibitor of leukotriene biosynthesis (IC50 = 3 nM in human polymorphonuclear leukocytes). Acts by inhibiting 5-lipoxygenase-activating protein (FLAP) (IC50 = 30 nM for inhibition of [125I]-L-691,678 photoaffinity labelling). Also moderately potent PPARα antagonist (IC50 = 0.5-1 μM). Orally active in vivo.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Data Sheet
Kehrer et al (2001) Inhibition of peroxisome-proliferator-activated receptor (PPAR)α by MK886. Biochem.J. 356 899. PMID: 11389700.
Mancini et al (1992) 5-Lipoxygenase-activating protein is the target of a novel hybrid of two classes of leukotriene biosynthesis inhibitors. Mol.Pharmacol. 41 267. PMID: 1538707.
Dixon et al (1990) Requirement of a 5-lipoxygenase-activating protein for leukotriene synthesis. Nature 343 282. PMID: 2300173.
Gillard et al (1989) L-663,536 (MK-886) (3-[1-(4-chlorobenzyl)-3-t-butyl-thio-5-isopropylindol-2-yl]-2,2-dimethylpropanoic acid), a novel, orally active leukotriene biosynthesis inhibitor. Can.J.Physiol.Pharmacol. 67 456. PMID: 2548691.
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Citations are publications that use Tocris products. Selected citations for MK 886 include:
Shahid et al (2015) Acinar Cell Production of Leukotriene B4 Contributes to Development of Neurogenic Pancreatitis in Mice. J Neuroinflammation 1 75. PMID: 25729765.
Rizvi et al (2013) Interactions of PPAR-alpha and adenosine receptors in hypoxia-induced angiogenesis. Vascul Pharmacol 59 144. PMID: 24050945.
Roversi et al (2013) Bifunctional lipocalin ameliorates murine immune complex-induced acute lung injury. J Biol Chem 288 18789. PMID: 23625922.
Scuderi et al (2012) Palmitoylethanolamide exerts neuroprotective effects in mixed neuroglial cultures and organotypic hippocampal slices via peroxisome proliferator-activated receptor-α. J Pharmacol Exp Ther 9 49. PMID: 22405189.
Esposito et al (2011) Cannabidiol reduces Aβ-induced neuroinflammation and promotes hippocampal neurogenesis through PPARγ involvement. Cell Mol Gastroenterol Hepatol 6 e28668. PMID: 22163051.
Mascia et al (2011) Blockade of nicotine reward and reinstatement by activation of alpha-type peroxisome proliferator-activated receptors. Biol Psychiatry 69 633. PMID: 20801430.
Melis et al (2008) Endogenous fatty acid ethanolamides suppress nicotine-induced activation of mesolimbic dopamine neurons through nuclear receptors. J Neurosci 28 13985. PMID: 19091987.
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Keywords: MK 886, supplier, Inhibitor, 5-lipoxygenase-activating, protein, FLAP, PPARα, PPARalpha, antagonists, inhibitors, inhibits, Oxygenases, Oxidases, leukotrienes, eicosanoids, biosynthesis, Peroxisome, Proliferator-activated, PPARs, MK886, L663536, 5-LOX, Tocris Bioscience, Lipoxygenase Inhibitor products
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