"目录号: HY-14166

Immunology/Inflammation-

MK886是一个强的FLAP抑制剂，也是非竞争的PPAR alpha的抑制剂。

FLAP

相关产品

MK591-GSK2190915-AM679-MK-0591-AM 103-

生物活性

Description

MK886 is a potent 5-lipoxygenase activating protein inhibitor (FLAP) also a non-competitive inhibitor of PPAR alpha. a potent inhibitor of leukotriene (LT) biosynthesis in intact human polymorphonuclear leukocytes with IC 50 of 2.5 nM. Block the synthessis of leukotrien intact activate leukocyte.target: FLAP, LTIC50: 2.5 nM ( leukotriene ,LT )In vitro: MK886 inhibit PPAR alpha by a non-competitive mechanism as shown by its effects on the binding of arachidonic acid to PPAR alpha protein. The expression of keratin-1 is reduced by MK886 in a culture of mouse primary keratinocytes. MK886 functioning as a non-competitive inhibitor of PPAR alpha, but may also indicate that PPAR alpha is not directly involved in MK886-induced apoptosis. In vivo: L-663,536 inhibit A23187-induced LTB4 formation by rat peripheral blood and elicited PMN. The compound inhibited leukotriene biosynthesis in vivo in a rat pleurisy model (ED50, 0.2 mg/kg p.o.), an inflamed rat paw model (ED50, 0.8 mg/kg)

References

[1].[1] Kehrer JP et al. Inhibition of peroxisome-proliferator-activated receptor (PPAR)alpha by MK886. Biochem J. 2001 Jun 15.

[2].[2] Gillard J et al. 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. 1989 May;67(5):456-64.

[3].[3] Dixon RA et al. Requirement of a 5-lipoxygenase-activating protein for leukotriene synthesis. Nature, 1990 Jan 18, 343(6255):282-4.  http://www.ncbi.nlm.nih.gov/pubmed/2300173