MK 886

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Description: Inhibitor of 5-lipoxygenase-activating protein (FLAP)
Alternative Names: L-663,536
Chemical Name: 1-[(4-Chlorophenyl)methyl]-3-[(1,1-dimethylethyl)thio]-α,α-dimethyl-5-(1-methylethyl)-1H-Indole-2-propanoic acid
Purity: ≥98% (HPLC)
Citations (11)

Biological Activity for MK 886

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 for MK 886

M. Wt 472.08
Formula C27H34ClNO2S
Storage Store at RT
Purity ≥98% (HPLC)
CAS Number 118414-82-7
PubChem ID 3651377
Smiles ClC(C=C3)=CC=C3CN(C(CC(C)(C(O)=O)C)=C2SC(C)(C)C)C1=C2C=C(C(C)C)C=C1

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.

Solubility Data for MK 886

Solvent Max Conc. mg/mL Max Conc. mM
ethanol 2.36 5
DMSO 47.21 100

Preparing Stock Solutions for MK 886

The following data is based on the product molecular weight 472.08. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.12 mL 10.59 mL 21.18 mL
5 mM 0.42 mL 2.12 mL 4.24 mL
10 mM 0.21 mL 1.06 mL 2.12 mL
50 mM 0.04 mL 0.21 mL 0.42 mL

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Product Datasheets for MK 886

Certificate of Analysis / Product Datasheet
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References for MK 886

References are publications that support the biological activity of the product.

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

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

If you know of a relevant reference for MK 886, please let us know.

View Related Products by Product Action

View all Lipoxygenase Inhibitors

Keywords: MK 886, 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, L-663,536, Lipoxygenase, Receptors, Leukotriene, and, Related, 1311, Tocris Bioscience

11 Citations for MK 886

Citations are publications that use Tocris products. Selected citations for MK 886 include:

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

Rizvi et al (2013) Interactions of PPAR-alpha and adenosine receptors in hypoxia-induced angiogenesis. Vascul Pharmacol 59 144 PMID: 24050945

Do you know of a great paper that uses MK 886 from Tocris? Please let us know.

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