[CAS NO. 118414-82-7] MK-886

Name: MK-886
Brand: Arctom Scientific
SKU: SLK-S8236

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PRODUCTS SPECIFICATIONS [118414-82-7]

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Catalog

SLK-S8236

Brand

Selleck

CAS

118414-82-7

DESCRIPTION [118414-82-7]

Overview

MDL	MFCD00876710
Molecular Weight	472.08
Molecular Formula	C27H34ClNO2S
SMILES	C(N1C=2C(C(SC(C)(C)C)=C1CC(C(O)=O)(C)C)=CC(C(C)C)=CC2)C3=CC=C(Cl)C=C3

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.1183 mL	10.5914 mL	21.1829 mL
5 mM	0.4237 mL	2.1183 mL	4.2366 mL
10 mM	0.2118 mL	1.0591 mL	2.1183 mL
50 mM	0.0424 mL	0.2118 mL	0.4237 mL

Description

MK-886 is an inhibitor of , inhibiting . It is also a moderately potent .

Targets

5-lipoxygenase-activating protein (FLAP) ^[1]	PPARα ^[3]	COX-1 ^[1]	COX-2 ^[1]
		8 μM	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. MK-886 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, MK-886 (33 μM) failed to suppress COX-2-dependent 6-ketoprostaglandin (PG)F1α formation. MK-886 (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.

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 MK-886 does not alter cortical GluR1 phosphorylation.

References

[1] Koeberle A, et al. Eur J Pharmacol. 2009, 608(1-3):84-90.
[2] Imbesi M, et al. Brain Res. 2007, 1147:148-53.
[3] Kehrer JP, et al. Biochem J. 2001, 356(Pt 3):899-906.

Synonyms

1H-Indole-2-propanoic acid, 1-[(4-chlorophenyl)methyl]-3-[(1,1-dimethylethyl)thio]-α,α-dimethyl-5-(1-methylethyl)-

1-[(4-Chlorophenyl)methyl]-3-[(1,1-dimethylethyl)thio]-α,α-dimethyl-5-(1-methylethyl)-1H-indole-2-propanoic acid

L 663536

MK 886