1. Immunology/Inflammation
    GPCR/G Protein
    Cell Cycle/DNA Damage
    Apoptosis
  2. FLAP
    Leukotriene Receptor
    PPAR
    Apoptosis
  3. MK-886

MK-886 (Synonyms: L 663536)

Cat. No.: HY-14166 Purity: 99.77%
Handling Instructions

MK-886 (L 663536) is a potent, cell-permeable and orally active FLAP (IC50 of 30 nM) and leukotriene biosynthesis (IC50s of 3 nM and 1.1 μM in intact leukocytes and human whole blood, respectively) inhibitor. MK-886 is also a non-competitive PPARα antagonist and can induce apoptosis.

For research use only. We do not sell to patients.

MK-886 Chemical Structure

MK-886 Chemical Structure

CAS No. : 118414-82-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 92 In-stock
Estimated Time of Arrival: December 31
5 mg USD 84 In-stock
Estimated Time of Arrival: December 31
10 mg USD 144 In-stock
Estimated Time of Arrival: December 31
25 mg USD 288 In-stock
Estimated Time of Arrival: December 31
50 mg USD 528 In-stock
Estimated Time of Arrival: December 31
100 mg USD 756 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Description

MK-886 (L 663536) is a potent, cell-permeable and orally active FLAP (IC50 of 30 nM) and leukotriene biosynthesis (IC50s of 3 nM and 1.1 μM in intact leukocytes and human whole blood, respectively) inhibitor. MK-886 is also a non-competitive PPARα antagonist and can induce apoptosis[1][2][3].

IC50 & Target

IC50: 30 nM (FLAP)[3]
IC50: 3 nM (Leukotriene biosynthesis in intact leukocytes) and 1.1 μM (Leukotriene biosynthesis in human whole blood)[2]
PPARα[1]

In Vitro

MK-886 (0.5-2 µM; 15 hours; primary keratinocytes) treatment reduces keratin-1 expression in a culture of mouse primary keratinocytes[1].
Using a transient transfection system in monkey kidney fibroblast CV-1 cells, mouse keratinocyte 308 cells and human lung adenocarcinoma A549 cells, 10 µM MK-886 is able to inhibit Wy-14643 activation of PPARα by ~80%. MK-886 also decreases PPARα activation by fatty acids in the stable transfection system[1].
Although Jurkat cells express all PPAR isoforms, various PPARα and PPARγ agonists are unable to prevent MK-886-induced apoptosis[1].

Western Blot Analysis[1]

Cell Line: Primary keratinocytes
Concentration: 0.5 µM, 1 µM or 2 µM
Incubation Time: 15 hours
Result: Decreased in keratin-1 expression.
In Vivo

MK-886 (L 663536; 5 mg/kg; oral administration; male Sprague-Dawley rats) treatment potently inhibits the antigen-induced dyspnea in inbred rats pretreated with methysergide[2].
MK-886 (L 663536) inhibits leukotriene biosynthesis in vivo in a rat pleurisy model (ED50, 0.2 mg/kg p.o.), an inflamed rat paw model (ED50, 0.8 mg/kg), a model of leukotriene excretion in rat bile following antigen provocation[2].

Animal Model: Male Sprague-Dawley rats (300-400 g) with antigen-induced dyspnea[1]
Dosage: 5 mg/kg
Administration: Oral administration
Result: Inhibited the antigen-induced dyspnea.
Molecular Weight

472.08

Formula

C₂₇H₃₄ClNO₂S

CAS No.

118414-82-7

SMILES

CC(C)C1=CC=C(N(CC2=CC=C(Cl)C=C2)C(CC(C)(C(O)=O)C)=C3SC(C)(C)C)C3=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 32 mg/mL (67.79 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1183 mL 10.5914 mL 21.1828 mL
5 mM 0.4237 mL 2.1183 mL 4.2366 mL
10 mM 0.2118 mL 1.0591 mL 2.1183 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  0.5% CMC-Na/saline water

    Solubility: 10 mg/mL (21.18 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (5.30 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.30 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

MK-886L 663536MK886MK 886L663536L-663536FLAPLeukotriene ReceptorPPARApoptosis5-lipoxygenase-activating protein5-LO activating proteinPeroxisome proliferator-activated receptorsPPARαnon-competitiveapoptosiskeratin-15-LOXleukotrienebiosynthesisInhibitorinhibitorinhibit

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MK-886
Cat. No.:
HY-14166
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