R&D Systems Inc. Tocris Bioscience Boston Biochem

MK 886

Cat. No. 1311

MK 886 C27H34ClNO2S [118414-82-7]

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Alternative Name: 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

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
Solubility:
Soluble to 5 mM in ethanol and to 100 mM in DMSO
Purity:
>98 %
Storage:
Store at RT
CAS No:
118414-82-7

The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.

Resources

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch
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Safety Data Sheet: View Safety Data Sheet

References

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.

Dixon et al (1990) Requirement of a 5-lipoxygenase-activating protein for leukotriene synthesis. Nature 343 282. PMID: 2300173.

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.

Kehrer et al (2001) Inhibition of peroxisome-proliferator-activated receptor (PPAR)α by MK886. Biochem.J. 356 899. PMID: 11389700.

If you know of a relevant citation for this product please let us know.

View Related Products by Target

Leukotriene and Related Receptors Lipoxygenase Oxygenases/Oxidases
PPAR PPARα

Keywords: MK 886, supplier, Inhibitor, 5-lipoxygenase-activating, protein, FLAP, PPARα, PPARalpha, antagonists, inhibitors, Oxygenases, Oxidases, leukotrienes, eicosanoids, biosynthesis, Peroxisome, Proliferator-activated, PPARs, MK886, L663536, 5-LOX

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