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Submit ReviewMK 886 is a potent inhibitor of 5-lipoxygenase-activating protein (FLAP) (IC50 = 30 nM for inhibition of [125I]-L-691,678 photoaffinity labelling). Inhibits leukotriene biosynthesis (IC50 = 3 nM in human polymorphonuclear leukocytes). Also moderately potent PPARα antagonist (IC50 = 0.5-1 μM). Orally active in vivo.
分子量 | 472.08 |
公式 | C27H34ClNO2S |
储存 | Store at RT |
纯度 | ≥98% (HPLC) |
CAS Number | 118414-82-7 |
PubChem ID | 3651377 |
InChI Key | QAOAOVKBIIKRNL-UHFFFAOYSA-N |
Smiles | ClC(C=C3)=CC=C3CN(C(CC(C)(C(O)=O)C)=C2SC(C)(C)C)C1=C2C=C(C(C)C)C=C1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
ethanol | 2.36 | 5 | |
DMSO | 47.21 | 100 |
以下数据基于产品分子量 472.08。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.12 mL | 10.59 mL | 21.18 mL |
5 mM | 0.42 mL | 2.12 mL | 4.24 mL |
10 mM | 0.21 mL | 1.06 mL | 2.12 mL |
50 mM | 0.04 mL | 0.21 mL | 0.42 mL |
参考文献是支持产品生物活性的出版物。
Dixon et al (1990) Requirement of a 5-lipoxygenase-activating protein for leukotriene synthesis. Nature 343 282 PMID: 2300173
Gillard et al (1989) 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. 67 456 PMID: 2548691
Kehrer et al (2001) Inhibition of peroxisome-proliferator-activated receptor (PPAR)α by MK886. Biochem.J. 356 899 PMID: 11389700
Mancini et al (1992) 5-Lipoxygenase-activating protein is the target of a novel hybrid of two classes of leukotriene biosynthesis inhibitors. Mol.Pharmacol. 41 267 PMID: 1538707
If you know of a relevant reference for MK 886, please let us know.
关键词: MK 886, MK 886 supplier, Inhibitor, 5-lipoxygenase-activating, protein, FLAP, PPARα, PPARalpha, antagonists, inhibitors, inhibits, Oxygenases, Oxidases, leukotrienes, eicosanoids, biosynthesis, Peroxisome, Proliferator-activated, PPARs, MK886, L663536, 5-LOX, L-663,536, Lipoxygenase, Receptors, Leukotriene, and, Related, 1311, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 MK 886 的部分引用包括:
Oguh-Olayinka et al (2019) The Investigation of Lipoxygenases as Therapeutic Targets in Malignant Pleural Mesothelioma. Pathol Oncol Res PMID: 30941737
Eisele et al (2013) The peroxisome proliferator-activated receptor γ coactivator 1α/β (PGC-1) coactivators repress the transcriptional activity of NF-κB in skeletal muscle cells. J Biol Chem 288 2246 PMID: 23223635
Puligheddu et al (2013) PPAR-alpha agonists as novel antiepileptic drugs: preclinical findings. PLoS One 8 e64541 PMID: 23724059
Shahid et al (2015) Acinar Cell Production of Leukotriene B4 Contributes to Development of Neurogenic Pancreatitis in Mice. J Neuroinflammation 1 75 PMID: 25729765
Scuderi et al (2012) Palmitoylethanolamide exerts neuroprotective effects in mixed neuroglial cultures and organotypic hippocampal slices via peroxisome proliferator-activated receptor-α. J Pharmacol Exp Ther 9 49 PMID: 22405189
Esposito et al (2011) Cannabidiol reduces Aβ-induced neuroinflammation and promotes hippocampal neurogenesis through PPARγ involvement. Cell Mol Gastroenterol Hepatol 6 e28668 PMID: 22163051
Mascia et al (2011) Blockade of nicotine reward and reinstatement by activation of alpha-type peroxisome proliferator-activated receptors. Biol Psychiatry 69 633 PMID: 20801430
Rizvi et al (2013) Interactions of PPAR-alpha and adenosine receptors in hypoxia-induced angiogenesis. Vascul Pharmacol 59 144 PMID: 24050945
Roversi et al (2013) Bifunctional lipocalin ameliorates murine immune complex-induced acute lung injury. J Biol Chem 288 18789 PMID: 23625922
Vigna et al (2011) Leukotriene B4 mediates inflammation via TRPV1 in duct obstruction-induced pancreatitis in rats. Pancreas 40 708 PMID: 21602738
Melis et al (2008) Endogenous fatty acid ethanolamides suppress nicotine-induced activation of mesolimbic DA neurons through nuclear receptors. J Neurosci 28 13985 PMID: 19091987
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