Catalog Number: 1311
Alternate Names: L-663,536
Chemical Name: 1-[(4-Chlorophenyl)methyl]-3-[(1,1-dimethylethyl)thio]-α,α-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.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 5 mM in ethanol and to 100 mM in DMSO
  • Purity:
  • Storage:
    Store at RT
  • CAS No:
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Inhibition of peroxisome-proliferator-activated receptor (PPAR)α by MK886.
    Kehrer et al.
    Biochem.J., 2001;356:899
  2. 5-Lipoxygenase-activating protein is the target of a novel hybrid of two classes of leukotriene biosynthesis inhibitors.
    Mancini et al.
    Mol.Pharmacol., 1992;41:267
  3. Requirement of a 5-lipoxygenase-activating protein for leukotriene synthesis.
    Dixon et al.
    Nature, 1990;343:282
  4. 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.
    Gillard et al.
    Can.J.Physiol.Pharmacol., 1989;67:456
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