MK-886 (L 663536) is a potent, cell-permeable and orally active FLAP (IC50 of 30 nM) and leukotriene biosynthesis (IC50 s of 3 nM and 1.1 μM in intact leukocytes and human whole blood, respectively) inhibitor. MK-886 is also a non-competitive PPARα antagonist and can induce apoptosis [1] [2] [3].

MK-886, or L-663536, is a leukotriene antagonist. It may perform this by blocking the 5-lipoxygenase activating protein (FLAP), thus inhibiting 5-lipoxygenase (5-LOX), [1] and may help in treating atherosclerosis.

MK-886: 一种FLAP抑制剂、PPARα抑制剂药物，由Merck Sharp & Dohme Corp. (Merck Sharp & Dohme Corp.)公司最早进行研发，目前全球最高研发状态为临床前，作用机制: FLAP抑制剂 (5-脂氧合酶激活蛋白抑制剂),PPARα抑制剂 (过氧化物酶体增长因子活化受体α抑制剂)，治疗领域: 免疫 ...

2009年4月17日 · MK-886, an inhibitor of the 5-lipoxygenase-activating protein (FLAP), potently suppresses leukotriene biosynthesis in intact cells and is frequently used to define a role of the 5-lipoxygenase (EC 1.13.11.34) pathway in cellular or animal models of inflammation, allergy, cancer, and cardiovascular disease.

MK-886 (L 663536) is a potent, cell-permeable and orally active FLAP (IC50 of 30 nM) and leukotriene biosynthesis (IC50 s of 3 nM and 1.1 μM in intact leukocytes and human whole blood, respectively) inhibitor. MK-886 is also a non-competitive PPARα antagonist and can induce apoptosis [1][2][3].

MK 886 is a potent inhibitor of 5-lipoxygenase-activating protein (FLAP) (IC 50 = 30 nM for inhibition of [125 I]-L-691,678 photoaffinity labelling). Inhibits leukotriene biosynthesis (IC 50 = 3 nM in human polymorphonuclear leukocytes).

MK-886是一种白三烯生物合成的抑制剂，能够抑制5-脂氧合酶激活蛋白（FLAP）。 此外，MK-886还是PPARα的拮抗剂。 产品性质

MK 886 is a potent inhibitor of 5-lipoxygenase-activating protein (FLAP) (IC 50 = 30 nM for inhibition of [125 I]-L-691,678 photoaffinity labelling). Inhibits leukotriene biosynthesis (IC 50 = 3 nM in human polymorphonuclear leukocytes).

MK-886 (L 663536) sodium salt is a potent, cell-permeable and orally active FLAP (IC50 of 30 nM) and leukotriene biosynthesis (IC50 s of 3 nM and 1.1 μM in intact leukocytes and human whole blood, respectively) inhibitor. MK-886 sodium salt is also a non-competitive PPARα antagonist and can induce apoptosis [1] [2] [3].