Powder: -20°C for 3 years | In solvent: -80°C for 1 year
MK-886 (L 663536)是一种细胞可渗透的,具有口服活性的 FLAP (IC50为 30 nM) 和白三烯生物合成 (完整白细胞和人全血中的IC50分别为 3 nM 和 1.1μM) 的抑制剂。它也是一种非竞争性PPARα拮抗剂,可以诱导细胞凋亡。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 248 | 现货 | ||
2 mg | ¥ 356 | 现货 | ||
5 mg | ¥ 578 | 现货 | ||
10 mg | ¥ 980 | 现货 | ||
25 mg | ¥ 1,890 | 现货 | ||
50 mg | ¥ 3,120 | 现货 | ||
100 mg | ¥ 4,590 | 现货 | ||
500 mg | ¥ 9,670 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 590 | 现货 |
产品描述 | MK-886 (L 663536) is an inhibitor of leukotriene biosynthesis, inhibiting 5-lipoxygenase-activating protein (FLAP). It is also a moderately potent PPARα antagonist. |
靶点活性 | COX-2:58 μM, COX-1:8 μM |
体外活性 | 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]. |
体内活性 | 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]. |
激酶实验 | Enzyme assay is conducted in buffer containing 25 mM Tris, pH 8.0, 1 mM DTT, 1 mM spermine, 50 mM KCl, 0.01% Nonidet P-40, and 1 mM MgCl2. PARP reaction contains 0.1 μCi [3H]NAD+ (200 000 DPM), 1.5 μM NAD+, 150 nM biotinylated NAD+, 1 μg/mL activated calf thymus, and 1?5 nM PARP-1. Autoreactions utilizing SPA bead-based detection are carried out in 50 μL volumes in white 96-well plates. Compounds (e.g., MK-4827) are prepared in 11-point serial dilution in 96-well plate, 5 μL/well in 5% DMSO/Water (10× concentrated). Reactions are initiated by adding first 35 μL of PARP-1 enzyme in buffer and incubating for 5 min at room temperature and then 10 μL of NAD+ and DNA substrate mixture. After 3 h at room temperature, these reactions are terminated by the addition of 50 μL of streptavidin-SPA beads (2.5 mg/mL in 200 mM EDTA, pH 8). After 5 min, they are counted using a TopCount microplate scintillation counter. IC50 data is determined from inhibition curves at various substrate concentrations[1]. |
细胞实验 | 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. (Only for Reference) |
别名 | MK886, L 663536 |
分子量 | 472.08 |
分子式 | C27H34ClNO2S |
CAS No. | 118414-82-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 2.4 mg/mL (5 mM)
DMSO: 47.2 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 2.1183 mL | 10.5914 mL | 21.1829 mL | 52.9571 mL |
5 mM | 0.4237 mL | 2.1183 mL | 4.2366 mL | 10.5914 mL | |
DMSO | 10 mM | 0.2118 mL | 1.0591 mL | 2.1183 mL | 5.2957 mL |
20 mM | 0.1059 mL | 0.5296 mL | 1.0591 mL | 2.6479 mL | |
50 mM | 0.0424 mL | 0.2118 mL | 0.4237 mL | 1.0591 mL | |
100 mM | 0.0212 mL | 0.1059 mL | 0.2118 mL | 0.5296 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
MK-886 118414-82-7 Apoptosis DNA Damage/DNA Repair GPCR/G Protein Immunology/Inflammation Metabolism Neuroscience Leukotriene Receptor COX PPAR FLAP leukotriene 5-LOX 5-LO activating protein non-competitive keratin-1 Inhibitor L-663536 biosynthesis Peroxisome proliferator-activated receptors PPARα MK 886 L663536 inhibit MK886 L 663536 inhibitor