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MK 886

Catalog No.
B6684
A FLAP and PPARα inhibitor, capable of inhibiting leukotriene biosynthesis and inducing apoptosis
Grouped product items
SizePriceStock Qty
5mg
$88.00
In stock
10mg
$158.00
In stock
25mg
$347.00
Ship with 5-10 days

Tel: +1-832-696-8203

Email: [email protected]

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Background

MK 886 is a potent, cell-permeable and orally-active inhibitor of 5-lipoxygenase-activating protein (FLAP), with an IC50 value of 30 nM for inhibition of [125I]-L-691,678 photoaffinity labelling. FLAP is essential for the activation of 5-lipoxygenase (5-LO) and therefore for the biosynthesis of leukotrienes. Leukotrienes, the biologically active metabolites of arachidonic acid, have been implicated in various inflammatory responses, such as asthma, arthritis as well as psoriasis. In addition, MK 886 is also a non-competitive antagonist of the peroxisome-proliferator-activated receptor alpha (PPARα), with the ability to induce apoptosis. 

References:

1. Mancini JA, Prasit P, Coppolino MG, et al. 5-Lipoxygenase-activating protein is the target of a novel hybrid of two classes of leukotriene biosynthesis inhibitors. Molecular Pharmacology, 1992, 41(2): 267-272.

2. Dixon RA, Diehl RE, Opas E, et al. Requirement of a 5-lipoxygenase-activating protein for leukotriene synthesis. Nature, 1990, 343(6255): 282-284.

3. Kehrer JP, Biswal SS, La E, et al. Inhibition of peroxisome-proliferator-activated receptor (PPAR)alpha by MK886. Biochemical Journal, 2001, 356(Pt 3): 899-906.

4. Imbesi M, Zavoreo I, Uz T, et al. 5-Lipoxygenase inhibitor MK-886 increases GluR1 phosphorylation in neuronal cultures in vitro and in the mouse cortex in vivo. Brain Research, 2007, 1147: 148-153.

Product Citation

Chemical Properties

Physical AppearanceWhite solid
StorageStore at RT
M.Wt472.08
Cas No.118414-82-7
FormulaC27H34ClNO2S
Solubility≥15.1 mg/mL in DMSO with ultrasonic; ≥2.16 mg/mL in EtOH with ultrasonic; insoluble in H2O
Chemical Name3-(3-(tert-butylthio)-1-(4-chlorobenzyl)-5-isopropyl-1H-indol-2-yl)-2,2-dimethylpropanoic acid
SDFDownload SDF
Canonical SMILESClC1=CC=C(C=C1)CN(C2=CC=C(C(C)C)C=C32)C(CC(C)(C(O)=O)C)=C3SC(C)(C)C
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Protocol

Cell experiment:[2]

Cell lines

Osteosarcoma cells expressing 5-LO, 5-LO and rat FLAP (5-LO/FLAP), or rat neutrophils

Reaction Conditions

0.3 μM MK 886 for osteosarcoma cells and 0.2 μM MK 886 for rat neutrophils

Applications

MK 886 blocked leukotriene synthesis both in the 5-LO/FLAP cell line and in neutrophils. MK 886 was able to inhibit the synthesis of leukotrienes in intact activated leukocytes, but showed little or no effect on enzymes directly involved in leukotriene synthesis, including 5-LO.

Animal experiment:[4]

Animal models

Male C57BL/6J mice

Dosage form

3 mg/kg

Intraperitoneal (i.p.) injection

Applications

Repeated daily i.p. injections of MK 886 increased phosphorylation of AMPAR subunit glutamate receptor 1 (GluR1) in brain samples obtained from the prefrontal cortex, whereas a single injection of MK 886 did not alter cortical GluR1 phosphorylation.

Note

The technical data provided above is for reference only.

References:

1. Mancini JA, Prasit P, Coppolino MG, et al. 5-Lipoxygenase-activating protein is the target of a novel hybrid of two classes of leukotriene biosynthesis inhibitors. Molecular Pharmacology, 1992, 41(2): 267-272.

2. Dixon RA, Diehl RE, Opas E, et al. Requirement of a 5-lipoxygenase-activating protein for leukotriene synthesis. Nature, 1990, 343(6255): 282-284.

3. Kehrer JP, Biswal SS, La E, et al. Inhibition of peroxisome-proliferator-activated receptor (PPAR)alpha by MK886. Biochemical Journal, 2001, 356(Pt 3): 899-906.

4. Imbesi M, Zavoreo I, Uz T, et al. 5-Lipoxygenase inhibitor MK-886 increases GluR1 phosphorylation in neuronal cultures in vitro and in the mouse cortex in vivo. Brain Research, 2007, 1147: 148-153.

Quality Control

Chemical structure

MK 886

Related Biological Data

MK 886