MK 886
Chemical Name: 1-[(4-Chlorophenyl)methyl]-3-[(1,1-dimethylethyl)thio]-α,α-dimethyl-5-(1-methylethyl)-1H-Indole-2-propanoic acid
Purity: ≥98%
Biological Activity
MK 886 is a potent inhibitor of 5-lipoxygenase-activating protein (FLAP) (IC50 = 30 nM for inhibition of [125I]-L-691,678 photoaffinity labelling). Inhibits leukotriene biosynthesis (IC50 = 3 nM in human polymorphonuclear leukocytes). Also moderately potent PPARα antagonist (IC50 = 0.5-1 μM). Orally active in vivo.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Requirement of a 5-lipoxygenase-activating protein for leukotriene synthesis.
Dixon et al.
Nature, 1990;343:282 -
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.
Gillard et al.
Can.J.Physiol.Pharmacol., 1989;67:456 -
Inhibition of peroxisome-proliferator-activated receptor (PPAR)α by MK886.
Kehrer et al.
Biochem.J., 2001;356:899 -
5-Lipoxygenase-activating protein is the target of a novel hybrid of two classes of leukotriene biosynthesis inhibitors.
Mancini et al.
Mol.Pharmacol., 1992;41:267
Product Datasheets
Citations for MK 886
The citations listed below are publications that use Tocris products. Selected citations for MK 886 include:
11 Citations: Showing 1 - 10
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The Investigation of Lipoxygenases as Therapeutic Targets in Malignant Pleural Mesothelioma.
Authors: Oguh-Olayinka Et al.
Pathol Oncol Res 2019;
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Acinar Cell Production of Leukotriene B4 Contributes to Development of Neurogenic Pancreatitis in Mice.
Authors: Shahid Et al.
J Neuroinflammation 2015;1:75
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PPAR-alpha agonists as novel antiepileptic drugs: preclinical findings.
Authors: Puligheddu Et al.
PLoS One 2013;8:e64541
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Interactions of PPAR-alpha and adenosine receptors in hypoxia-induced angiogenesis.
Authors: Rizvi Et al.
Vascul Pharmacol 2013;59:144
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The peroxisome proliferator-activated receptor γ coactivator 1α/β (PGC-1) coactivators repress the transcriptional activity of NF-κB in skeletal muscle cells.
Authors: Eisele Et al.
J Biol Chem 2013;288:2246
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Bifunctional lipocalin ameliorates murine immune complex-induced acute lung injury.
Authors: Roversi Et al.
J Biol Chem 2013;288:18789
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Palmitoylethanolamide exerts neuroprotective effects in mixed neuroglial cultures and organotypic hippocampal slices via peroxisome proliferator-activated receptor-α.
Authors: Scuderi Et al.
J Pharmacol Exp Ther 2012;9:49
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Cannabidiol reduces Aβ-induced neuroinflammation and promotes hippocampal neurogenesis through PPARγ involvement.
Authors: Esposito Et al.
Cell Mol Gastroenterol Hepatol 2011;6:e28668
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Blockade of nicotine reward and reinstatement by activation of alpha-type peroxisome proliferator-activated receptors.
Authors: Mascia Et al.
Biol Psychiatry 2011;69:633
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Leukotriene B4 mediates inflammation via TRPV1 in duct obstruction-induced pancreatitis in rats.
Authors: Vigna Et al.
Pancreas 2011;40:708
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Endogenous fatty acid ethanolamides suppress nicotine-induced activation of mesolimbic DA neurons through nuclear receptors.
Authors: Melis Et al.
J Neurosci 2008;28:13985
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