"目录号: HY-14166
MK886是一个强的FLAP抑制剂，也是非竞争的PPAR alpha的抑制剂。
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
