MK-886

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

MK-886 是一种白三烯生物合成抑制剂，可抑制 5-脂氧合酶激活蛋白 (FLAP)。它也是一种中等效力的 PPARα 拮抗剂。

MK-886 is an inhibitor of leukotriene biosynthesis, inhibiting 5-lipoxygenase-activating protein (FLAP). It is also a moderately potent PPARα antagonist.

MK-886 (0.5-2 μM; 15?hours; primary keratinocytes) treatment reduces keratin-1 expression in a culture of mouse primary keratinocytes.Using a transient transfection system in monkey kidney fibroblast CV-1 cells, mouse keratinocyte 308 cells and human lung adenocarcinoma A549 cells, 10 μM MK-886 is able to inhibit Wy-14643 activation of PPARα by ~80%. MK-886 also decreases PPARα activation by fatty acids in the stable transfection system.Although Jurkat cells express all PPAR isoforms, various PPARα and PPARγ agonists are unable to prevent MK-886-induced apoptosis. Western Blot Analysis Cell Line:Primary keratinocytes Concentration:0.5 μM, 1 μM or 2 μM Incubation Time:15?hours Result:Decreased in keratin-1 expression.

MK-886 (L 663536; 5 mg/kg; oral administration; male Sprague-Dawley rats) treatment potently inhibits the antigen-induced dyspnea in inbred rats pretreated with methysergide.MK-886 (L 663536) inhibits 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), a model of leukotriene excretion in rat bile following antigen provocation. Animal Model:Male Sprague-Dawley rats (300-400 g) with antigen-induced dyspnea Dosage:5 mg/kg Administration:Oral administration Result:Inhibited the antigen-induced dyspnea.

L 663536

Others

Other Targets

COX-1| COX-2

Cancer

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118414-82-7

472.08

C27H34ClNO2S

>98% (HPLC)

DMSO : ≥ 32 mg/mL 67.79 mM; H2O : < 0.1 mg/mL

CC(C)c1cc2c(cc1)n(c(c2SC(C)(C)C)CC(C)(C)C(=O)O)Cc1ccc(cc1)Cl

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(-20℃)

With Ice Pack

≥ 2 years