Biochem/physiol Actions

Reversible: no

Product does not compete with ATP.

Primary Targetleukotreine biosybthesis

Cell permeable: yes

General description

A cell-permeable, orally active NSAID (nonsteroidal antiinflammatory drug) that blocks cellular Cox pathway PGE2 (prostaglandin E₂) production by inhibiting COX-1 and mPGES-1 (microsomal PGE₂ synthase-1), but not COX-2, activity (IC₅₀ = 8, 2, and 58 M, respectively), as well as suppresses cellular 5-LO (5-Lypoxygenase; Cat. No. 437996) pathway activation by inhibiting FLAP (5-LO-activating protein), rather than 5-LO, activity (﹤10% by 1 M MK-886). Unlike NSAIDs (nonsteroidal antiinflammatory drugs) that target only COX pathway, MK-886 does not cause gastrointestinal damages when applied in vivo.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Koeberle, A., et al. 2009. Eur. J. Pharmacol.608, 84.Koeberle, A., et al. 2008. J. Pharmacol. Exp. Ther.326, 975.Fisher, L., et al. 2007. Br. J. Pharmacol.152, 471.Ford-Hutchinson, A.W., et al. 1993. Can. J. Physiol. Pharmacol. 71, 806.Ford-Hutchinson, A.W. 1991. Trends Pharmacol.12, 68.Dixon, R.A., et al. 1990. Nature 343, 282.Rouzer, C.A., et al. 1990. J. Biol. Chem.265, 1436.

Packaging

5 mg in Plastic ampoule

Warning

Toxicity: Standard Handling (A)