MK-886

Химические свойства

White Solid

Использование

MK-886 is a potent and selective inhibitor of FLAP and Cox-1.

Определение

ChEBI: A member of the class of indoles that is 1H-indole substituted by a isopropyl group at position 5, a tert-butylsulfanediyl group at position 3, a 4-chlorobenzyl group at position 1 and a 2-carboxy-2-methylpropyl group at pos tion 2. It acts as an inhibitor of arachidonate 5-lipoxygenase.

Биологическая активность

An inhibitor of leukotriene biosynthesis (IC 50 = 3 nM in human polymorphonuclear leukocytes). Acts by inhibiting 5-lipoxygenase-activating protein (FLAP) (IC 50 = 30 nM for inhibition of [ 125 I]-L-691,678 photoaffinity labelling). Also moderately potent PPAR α antagonist (IC 50 = 0.5-1 μ M). Orally active in vivo .