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MK-886 FLAP inhibitor

Name: MK-886
Brand: Selleck Chemicals
SKU: S8236
Availability: InStock
Rating: 5 (7 reviews)

Cat.No.S8236

MK-886 is an inhibitor of leukotriene biosynthesis, inhibiting 5-lipoxygenase-activating protein (FLAP). It is also a moderately potent PPARα antagonist.

Chemical Structure

Molecular Weight: 472.08

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability

Quality Control

Batch: S823601 DMSO]94 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.93%

99.93

Related Targets	Immunology & Inflammation related CD markers Interleukins Anti-infection Antioxidant COX Histamine Receptor TNF-alpha ROS Parasite PD-1/PD-L1 TLR Prostaglandin Receptor IFN CXCR Nrf2 NOS CCR NLRP3 eIF STING AhR IL Receptor Complement System IRAK β-lactamase IDO/TDO PGES NADPH-oxidase FKBP

Chemical Information, Storage & Stability

Molecular Weight	472.08	Formula	C₂₇H₃₄ClNO₂S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	118414-82-7	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	L-663,536			Smiles	CC(C)C1=CC2=C(C=C1)N(C(=C2SC(C)(C)C)CC(C)(C)C(=O)O)CC3=CC=C(C=C3)Cl

Solubility

In vitro
Batch:

DMSO : 94 mg/mL ( (199.11 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.350mg/ml (4.98mM)	Taking the 1 mL working solution as an example, add 50 μL of 47 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.780mg/ml (1.65mM)	Taking the 1 mL working solution as an example, add 50 μL of 15.6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	5-lipoxygenase-activating protein (FLAP) ^[1] PPARα ^[3] COX-1 ^[1] 8 μM COX-2 ^[1] 58 μM
In vitro	MK-886, an inhibitor of the 5-lipoxygenase-activating protein (FLAP), potently suppresses leukotriene biosynthesis in intact cells and is frequently used to define a role of the 5-lipoxygenase (EC 1.13.11.34) pathway in cellular or animal models of inflammation, allergy, cancer, and cardiovascular disease. This compound inhibits isolated COX-1 (IC50=8 μM) and blocks the formation of the COX-1-derived products 12(S)-hydroxy-5-cis-8,10-trans-heptadecatrienoic acid (12-HHT) and thromboxane B2 in washed human platelets in response to collagen as well as from exogenous arachidonic acid (IC50=13–15 μM).Isolated COX-2 was less affected (IC50=58 μM), and in A549 cells, this chemical (33 μM) failed to suppress COX-2-dependent 6-ketoprostaglandin (PG)F1α formation. It (10 μM) inhibits COX-1-mediated platelet aggregation induced by collagen or arachidonic acid whereas thrombin- or U-46619-induced (COX-independent) aggregation is not affected^[1].
In vivo	Repeated daily i.p. injections of MK-886 results in increased GluR1 phosphorylation in brain samples obtained from the prefrontal cortex. In contrast, a single injection of this compound does not alter cortical GluR1 phosphorylation^[2].
References	https://pubmed.ncbi.nlm.nih.gov/19239910/ https://pubmed.ncbi.nlm.nih.gov/17349982/ https://pubmed.ncbi.nlm.nih.gov/11389700/

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