化合物 MK886|T6893

MK-886
118414-82-7

￥248 1mg 起订

￥356 2mg 起订

￥578 5mg 起订

上海更新日期：2024-09-14

TargetMol中国（陶术生物）

VIP12年

联系人：邵小姐

电话：021-021-33632979拨打

手机：15002134094 拨打

邮箱：marketing@targetmol.com

产品详情:

中文名称：: 化合物 MK886

英文名称：: MK-886

CAS号：: 118414-82-7

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.78%

产品类别：: 抑制剂

货号：: T6893

Product Introduction

Bioactivity

Name	MK-886
Description	MK-886 (L 663536) is an inhibitor of leukotriene biosynthesis, inhibiting 5-lipoxygenase-activating protein (FLAP). It is also a moderately potent PPARα antagonist.
Cell Research	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)
Kinase Assay	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].
In vitro	MK-886是一种抑制5-脂氧合酶激活蛋白(FLAP)的化合物，能强效抑制完整细胞内的白三烯生物合成，常用于确定5-脂氧合酶(EC 1.13.11.34)途径在细胞或动物模型中对炎症、过敏、癌症和心血管疾病的作用。MK-886对分离的COX-1的抑制作用（IC50=8 µM），可以阻断由COX-1衍生的产物12(S)-羟基-5-顺-8,10-反-十七碳三烯酸(12-HHT)和血栓素B2在人类洗涤血小板中对胶原蛋白以及外源性花生四烯酸的响应中的形成（IC50=13–15 µM）。分离的COX-2受到的影响较小（IC50=58 µM），在A549细胞中，MK-886（33 µM）未能抑制COX-2依赖的6-酮前列腺素（PG）F1α的形成。MK-886（10 µM）能抑制COX-1介导的血小板聚集反应，该反应由胶原蛋白或花生四烯酸诱导，而由凝血酶或U-46619（COX独立）诱导的聚集并不受影响[1]。
In vivo	连续每日通过腹腔注射MK-886会增加从前额叶皮层获取的大脑样本中GluR1的磷酸化水平。相比之下，单次注射MK-886并不改变大脑皮质GluR1的磷酸化水平[2]。
Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
Solubility Information	Ethanol : 2.4 mg/mL (5 mM) DMSO : 55 mg/mL (116.51 mM)
Keywords	leukotriene \| FLAP \| 5-LOX \| 5-LO activating protein \| non-competitive \| keratin-1 \| Leukotriene Receptor \| Inhibitor \| L-663536 \| biosynthesis \| Peroxisome proliferator-activated receptors \| PPAR \| MK-886 \| PPARα \| MK 886 \| Apoptosis \| L663536 \| inhibit
Inhibitors Related	Daidzein \| Metronidazole \| 5-Fluorouracil \| Acetaminophen \| Stavudine \| Tributyrin \| Dextran sulfate sodium salt (MW 4500-5500) \| Myricetin \| Sorafenib \| L-Ascorbic acid \| Acetylcysteine \| Sodium 4-phenylbutyrate
Related Compound Libraries	Inhibitor Library \| Anti-Breast Cancer Compound Library \| Anti-Cancer Active Compound Library \| Bioactive Compound Library \| Bioactive Compounds Library Max \| Anti-Aging Compound Library \| Preclinical Compound Library \| GPCR Compound Library \| Membrane Protein-targeted Compound Library \| Pain-Related Compound Library

MK886|||L 663536|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子