MK 886 inhibits leukotriene biosynthesis (IC50 = 2.5 nM) in vitro and tumor activity in vivo. Displays PPARα antagonist activity. Orally active in vivo. MK-886, has been described that blocks the synthesis of leukotrienes in intact activated leukocytes, but has little or no effect on enzymes involved in leukotriene synthesis, including 5-lipoxygenase, in cell-free systems. MK 886 is a potent inhibitor of leukotriene biosynthesis both in vitro and in vivo indicating that the compound is suitable for studying the role of leukotrienes in a variety of pathological situations. MK 886 inhibited A23187-induced LTB4 formation by rat peripheral blood and elicited PMN.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 100 mg/mL
Ethanol 5 mg/mL
Inhibition of peroxisome-proliferator-activated receptor (PPAR)alpha by MK886.
Kehrer JP, et al. Biochem J. 2001 Jun 15;356(Pt 3):899-906. PMID: 11389700.
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 J, et al. Can J Physiol Pharmacol. 1989 May;67(5):456-64. PMID: 2548691.
Requirement of a 5-lipoxygenase-activating protein for leukotriene synthesis.
Dixon RA, et al. Nature. 1990 Jan 18;343(6255):282-4. PMID: 2300173.
5-Lipoxygenase-activating protein is the target of a novel hybrid of two classes of leukotriene biosynthesis inhibitors.
Mancini JA, et al. Mol Pharmacol. 1992 Feb;41(2):267-72. PMID: 1538707.
|Related Lipoxygenase Products|
GSK2190915 (AM803), a potent FLAP inhibitor, prevents the synthesis of leukotrienes and 5-oxo-ETE, with IC50 of 76 nM for inhibition of LTB4 in human blood, provides treatment for asthma.
Zileuton is an orally active 5-lipoxygenase (5-LOX) inhibitor that inhibits LTB4 synthesis with IC50 values of 0.56, 2.3 and 2.6 μM in dog, rat and human blood respectively.
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