MK-886

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Chemical Structure| 118414-82-7 同义名 : L 663536; L-663,536
CAS号 : 118414-82-7
货号 : A546613
分子式 : C27H34ClNO2S
纯度 : 99%+
分子量 : 472.08
MDL号 : MFCD00876710
存储条件：

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 80 mg/mL(169.46 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
靶点

  • lipoxygenase
描述 The 5-lipoxygenase-activating protein (FLAP), an integral membrane protein, facilitates substrate transfer to 5-lipoxygenase which catalyzes leukotriene formation from arachidonic acid, making it an alternative target (in addition to 5-lipoxygenase) to intervene with leukotriene biosynthesis and respective diseases. MK-886, a potent FLAP inhibitor, potently suppresses leukotriene biosynthesis in intact leukocytes with an IC50 of 2.5 nM. Moreover, MK-886 concentration-dependently inhibited COX-1 with an IC50 of 8 μM. In platelets, MK-886 concentration-dependently suppressed the formation of the COX-1-derived products 12-HHT and TxB2 with IC50 values of 13 – 15 μM. Further, 10 μM MK-886 decreased platelet aggregation in washed platelets evoked by collagen or arachidonic acid[3]. In vitro, MK-886 increased GluR1 phosphorylation at both serine 831 and serine 845. In vivo, repeated daily i.p. injections of MK-886 resulted in increased GluR1 phosphorylation in brain samples obtained from the prefrontal cortex supporting the use of MK-886 as a pharmacological tool in studies of not only the 5-LOX pathway but also neuronal GluR1 functioning[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.12mL

0.42mL

0.21mL

10.59mL

2.12mL

1.06mL

21.18mL

4.24mL

2.12mL
参考文献

[1]Kehrer JP, Biswal SS, et al. Inhibition of peroxisome-proliferator-activated receptor (PPAR)alpha by MK886. Biochem J. 2001 Jun 15;356(Pt 3):899-906.

[2]Gillard J, Ford-Hutchinson AW, 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]Koeberle A, Siemoneit U, et al. MK-886, an inhibitor of the 5-lipoxygenase-activating protein, inhibits cyclooxygenase-1 activity and suppresses platelet aggregation. Eur J Pharmacol. 2009 Apr 17;608(1-3):84-90

[4]Imbesi M, Zavoreo I, et al. 5-Lipoxygenase inhibitor MK-886 increases GluR1 phosphorylation in neuronal cultures in vitro and in the mouse cortex in vivo. Brain Res. 2007 May 25;1147:148-53