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Submit ReviewMK 886
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)
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 |
| 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 for MK 886
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| 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.
| 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
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.
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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:
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
Puligheddu et al (2013) PPAR-alpha agonists as novel antiepileptic drugs: preclinical findings. PLoS One 8 e64541 PMID: 23724059
Shahid et al (2015) Acinar Cell Production of Leukotriene B4 Contributes to Development of Neurogenic Pancreatitis in Mice. J Neuroinflammation 1 75 PMID: 25729765
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
Roversi et al (2013) Bifunctional lipocalin ameliorates murine immune complex-induced acute lung injury. J Biol Chem 288 18789 PMID: 23625922
Vigna et al (2011) Leukotriene B4 mediates inflammation via TRPV1 in duct obstruction-induced pancreatitis in rats. Pancreas 40 708 PMID: 21602738
Melis et al (2008) Endogenous fatty acid ethanolamides suppress nicotine-induced activation of mesolimbic DA neurons through nuclear receptors. J Neurosci 28 13985 PMID: 19091987
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