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 (11)
Reviews
Literature (2)

Biological Activity

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

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

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

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 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

Certificate of Analysis / Product Datasheet
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References

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:

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

Shahid et al (2015) Acinar Cell Production of Leukotriene B4 Contributes to Development of Neurogenic Pancreatitis in Mice. J Neuroinflammation 1 75 PMID: 25729765

Oguh-Olayinka et al (2019) The Investigation of Lipoxygenases as Therapeutic Targets in Malignant Pleural Mesothelioma. Pathol Oncol Res PMID: 30941737

Eisele et al (2013) The peroxisome proliferator-activated receptor γ coactivator 1α/β (PGC-1) coactivators repress the transcriptional activity of NF-κB in skeletal muscle cells. J Biol Chem 288 2246 PMID: 23223635


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