首页 工具
登录
购物车
MK-886

MK-886

产品编号 T6893   CAS 118414-82-7
别名: MK886, L 663536

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

TargetMol的所有产品和服务仅用于科学研究,不能被用于人体,我们也不向个人提供产品和服务。
MK-886 Chemical Structure
MK-886, CAS 118414-82-7
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
其他形式的 MK-886:
产品目录号及名称: MK-886 (T6893)
点击图片重新获取验证码
选择批次  
纯度: 99.23%
纯度: 98.9%
更多批次查询请联系客服
生物活性
化学信息
存储 & 溶解度
参考文献
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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: 2.4 mg/mL (5 mM)

DMSO: 47.2 mg/mL (100 mM)

溶液配制表

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

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
=
X
X
X
=
X
=
/
g/mol

输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Koeberle A, et al. Eur J Pharmacol. 2009, 608(1-3):84-90. 2. Imbesi M, et al. Brain Res. 2007, 1147:148-53. 3. Kehrer JP, et al. Biochem J. 2001, 356(Pt 3):899-906.

文献引用

1. Wang M, Luo W, Yu T, et al. Corynoline protects ang II-induced hypertensive heart failure by increasing PPARα and Inhibiting NF-κB pathway. Biomedicine & Pharmacotherapy. 2022, 150: 113075 2. Wang, Yuan, et al. Hippocampal PPARα plays a role in the pharmacological mechanism of vortioxetine, a multimodal-acting antidepressant. Frontiers in Pharmacology. 12 (2021). 3. Gao S, Zhang X, Xu H, et al. Promoting the hippocampal PPARα expression participates in the antidepressant mechanism of reboxetine, a selective norepinephrine reuptake inhibitor. Behavioural Brain Research. 2021: 113535. 4. Liang X, Liang J, Zhang S, et al.Di-2-ethylhexyl phthalate disrupts hepatic lipid metabolism in obese mice by activating the LXR/SREBP-1c and PPAR-α signaling pathways.Science of The Total Environment.2024: 169919.
Echinocystic acid GPNA hydrochloride Apoptozole SKI V Selumetinib 9-dihydro-13-acetylbaccatin III LYN-1604 EB-3D

相关化合物库

该产品包含在如下化合物库中:
抗癌活性化合物库 细胞焦亡化合物库 NO PAINS 化合物库 抗糖尿病库 代谢化合物库 GPCR靶点分子库 口服活性化合物库 DNA 损伤和修复分子库 抗肥胖化合物库 抗癌化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

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。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% ddH2O
计算 重置

技术支持

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。

Keywords

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

 

陶术
生物
TargetMol®中国区唯一合作伙伴
点击进入陶术生物官网陶术生物
联系我们
400-820-0310

上海市静安区江场三路238号8楼