MK-886

製品コードS8236 バッチS823601

印刷

化学情報

Chemical Structure Synonyms L-663,536 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C27H34ClNO2S
分子量 472.08 CAS No. 118414-82-7
Solubility (25°C)* 体外 DMSO 94 mg/mL (199.11 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 MK-886 is an inhibitor of leukotriene biosynthesis, inhibiting 5-lipoxygenase-activating protein (FLAP). It is also a moderately potent PPARα antagonist.
in vitro 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 inhibits isolated COX-1 (IC50=8 μM) and blocks the formation of the COX-1-derived products 12(S)-hydroxy-5-cis-8,10-trans-heptadecatrienoic acid (12-HHT) and thromboxane B2 in washed human platelets in response to collagen as well as from exogenous arachidonic acid (IC50=13–15 μM).Isolated COX-2 was less affected (IC50=58 μM), and in A549 cells, MK-886 (33 μM) failed to suppress COX-2-dependent 6-ketoprostaglandin (PG)F1α formation. MK-886 (10 μM) inhibits COX-1-mediated platelet aggregation induced by collagen or arachidonic acid whereas thrombin- or U-46619-induced (COX-independent) aggregation is not affected[1].
in vivo Repeated daily i.p. injections of MK-886 results in increased GluR1 phosphorylation in brain samples obtained from the prefrontal cortex. In contrast, a single injection of MK-886 does not alter cortical GluR1 phosphorylation[2].

プロトコル(参考用のみ)

細胞アッセイ 細胞株  A549 cells
濃度 33 μM
反応時間 15 min
実験の流れ

IL-1β-stimulated A549 cells (5×106/ml) are pre-incubated with MK-886 (MK, 33 μM), indomethacin (Indo, 10 μM), celecoxib (Cele, 5 μM) or vehicle (DMSO) for 15 min prior to the addition of 30 μM arachidonic acid. After 15 min at 37 °C, the amount of released 6-keto PGF1α was assessed by ELISA as described in the Materials and methods section.
動物実験 動物モデル Male C57BL/6J mice
投薬量 3 mg/kg
投与方法 i.p.

カスタマーフィードバック

Data from [Data independently produced by , , Eur J Pharmacol, 2018, 826:1-8]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

N-Palmitoyl-D-Glucosamine Inhibits TLR-4/NLRP3 and Improves DNBS-Induced Colon Inflammation through a PPAR-α-Dependent Mechanism [ Biomolecules, 2022, 12(8)1163] PubMed: 36009057
Sulfated glucuronomannan hexasaccharide G6S1 enhanced lipolysis and lipophagy via PPARα pathway [ Int J Biochem Cell Biol, 2021, 139:106067] PubMed: 34425199
The marine-derived furanone reduces intracellular lipid accumulation in vitro by targeting LXRα and PPARα [ J Cell Mol Med, 2020, 24(6):3384-3398] PubMed: 31981312
Bexarotene Exerts Protective Effects Through Modulation of the Cerebral Vascular Smooth Muscle Cell Phenotypic Transformation by Regulating PPARγ/FLAP/LTB4 After Subarachnoid Hemorrhage in Rats. [ Cell Transplant, 2019, 28(9-10):1161-1172] PubMed: 31010302
A novel PPARα/γ agonist, propane-2-sulfonic acid octadec-9-enyl-amide, ameliorates insulin resistance and gluconeogenesis in vivo and vitro [Ren T, et al. Eur J Pharmacol, 2018, 826:1-8] PubMed: 29476879
Corticosteroids inhibit anti-IgE activities of specialized proresolving mediators on B cells from asthma patients. [Kim N, et al. JCI Insight, 2017, 2(3):e88588] PubMed: 28194434

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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