MK 886

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MK 886

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

118414-82-7

包装与价格：

包装	价格(元)
5mg	电议
10mg	电议
25mg	电议

产品介绍

化学性质

Physical Appearance	White solid
Storage	Store at RT
M.Wt	472.08
Cas No.	118414-82-7
Formula	C₂₇H₃₄ClNO₂S
Solubility	≥15.1 mg/mL in DMSO with ultrasonic; ≥2.16 mg/mL in EtOH with ultrasonic; insoluble in H2O
Chemical Name	3-(3-(tert-butylthio)-1-(4-chlorobenzyl)-5-isopropyl-1H-indol-2-yl)-2,2-dimethylpropanoic acid
Canonical SMILES	ClC1=CC=C(C=C1)CN(C2=CC=C(C(C)C)C=C32)C(CC(C)(C(O)=O)C)=C3SC(C)(C)C
运输条件	蓝冰运输或根据您的需求运输。
一般建议	为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

MK 886 is a potent, cell-permeable and orally-active inhibitor of 5-lipoxygenase-activating protein (FLAP), with an IC50 value of 30 nM for inhibition of [125I]-L-691,678 photoaffinity labelling. FLAP is essential for the activation of 5-lipoxygenase (5-LO) and therefore for the biosynthesis of leukotrienes. Leukotrienes, the biologically active metabolites of arachidonic acid, have been implicated in various inflammatory responses, such as asthma, arthritis as well as psoriasis. In addition, MK 886 is also a non-competitive antagonist of the peroxisome-proliferator-activated receptor alpha (PPARα), with the ability to induce apoptosis.

References:

1. Mancini JA, Prasit P, Coppolino MG, et al. 5-Lipoxygenase-activating protein is the target of a novel hybrid of two classes of leukotriene biosynthesis inhibitors. Molecular Pharmacology, 1992, 41(2): 267-272.

2.Dixon RA, Diehl RE, Opas E, et al. Requirement of a 5-lipoxygenase-activating protein for leukotriene synthesis. Nature, 1990, 343(6255): 282-284.

3. Kehrer JP, Biswal SS, La E, et al. Inhibition of peroxisome-proliferator-activated receptor (PPAR)alpha by MK886. Biochemical Journal, 2001, 356(Pt 3): 899-906.

4. Imbesi M, Zavoreo I, Uz T, et al. 5-Lipoxygenase inhibitor MK-886 increases GluR1 phosphorylation in neuronal cultures in vitro and in the mouse cortex in vivo. Brain Research, 2007, 1147: 148-153.

试验操作

Cell experiment:[2]
Cell lines	Osteosarcoma cells expressing 5-LO, 5-LO and rat FLAP (5-LO/FLAP), or rat neutrophils
Reaction Conditions	0.3 μM MK 886 for osteosarcoma cells and 0.2 μM MK 886 for rat neutrophils
Applications	MK 886 blocked leukotriene synthesis both in the 5-LO/FLAP cell line and in neutrophils. MK 886 was able to inhibit the synthesis of leukotrienes in intact activated leukocytes, but showed little or no effect on enzymes directly involved in leukotriene synthesis, including 5-LO.
Animal experiment:[4]
Animal models	Male C57BL/6J mice
Dosage form	3 mg/kg Intraperitoneal (i.p.) injection
Applications	Repeated daily i.p. injections of MK 886 increased phosphorylation of AMPAR subunit glutamate receptor 1 (GluR1) in brain samples obtained from the prefrontal cortex, whereas a single injection of MK 886 did not alter cortical GluR1 phosphorylation.
Note	The technical data provided above is for reference only.
	References: 1. Mancini JA, Prasit P, Coppolino MG, et al. 5-Lipoxygenase-activating protein is the target of a novel hybrid of two classes of leukotriene biosynthesis inhibitors. Molecular Pharmacology, 1992, 41(2): 267-272. 2.Dixon RA, Diehl RE, Opas E, et al. Requirement of a 5-lipoxygenase-activating protein for leukotriene synthesis. Nature, 1990, 343(6255): 282-284. 3. Kehrer JP, Biswal SS, La E, et al. Inhibition of peroxisome-proliferator-activated receptor (PPAR)alpha by MK886. Biochemical Journal, 2001, 356(Pt 3): 899-906. 4. Imbesi M, Zavoreo I, Uz T, et al. 5-Lipoxygenase inhibitor MK-886 increases GluR1 phosphorylation in neuronal cultures in vitro and in the mouse cortex in vivo. Brain Research, 2007, 1147: 148-153.