Chemical Name:1-[(4-Chlorophenyl)methyl]-3-[(1,1-dimethylethyl)thio]-
a,a-dimethyl-5-(1-methylethyl)-1H-Indole-2-propanoic
acid
Biological Activity:
An inhibitor of leukotriene biosynthesis (IC50 = 3 nM
in human polymorphonuclear leukocytes). Acts by inhibiting
5-lipoxygenase-activating protein (FLAP) (IC50 = 30 nM for
inhibition of [125I]-L-691,678 photoaffinity labelling). Also
moderately potent PPARα antagonist (IC50
= 0.5-1 μM). Orally active in
vivo.
Gillardet al (1989) L-663,536 (MK-886)
(3-[1-(4-chlorobenzyl)-3-t-butyl-thio-5-isopropylindol-2-yl]-2,2-dimethylpropanoic
acid), a novel, orally active leukotriene biosynthesis inhibitor.
Can.J.Physiol.Pharmacol. 67 456. Dixonet al (1990)
Requirement of a 5-lipoxygenase-activating protein for leukotriene synthesis.
Nature 343 282. Manciniet al (1992)
5-Lipoxygenase-activating protein is the target of a novel hybrid of two
classes of leukotriene biosynthesis inhibitors. Mol.Pharmacol. 41
267. Kehreret al (2001) Inhibition of
peroxisome-proliferator-activated receptor (PPAR)α by MK886. Biochem.J. 356
899.
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