MK 886

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Cat.No. 1311 - MK 886 | C27H34ClNO2S | CAS No. 118414-82-7
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)
Datasheet
Citations (7)
Literature

Biological Activity

An 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.

Technical Data

M. Wt 472.08
Formula C27H34ClNO2S
Storage Store at RT
Purity ≥98% (HPLC)
CAS Number 118414-82-7
PubChem ID 3651377
InChI Key QAOAOVKBIIKRNL-UHFFFAOYSA-N
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

The following data is based on the product molecular weight 472.08. Batch specific molecular weights may vary from batch to batch due to solvent 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

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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, 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, Tocris Bioscience

7 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

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

Esposito et al (2011) Cannabidiol reduces Aβ-induced neuroinflammation and promotes hippocampal neurogenesis through PPARγ involvement. Cell Mol Gastroenterol Hepatol 6 e28668 PMID: 22163051

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

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


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