MK-886(Synonyms: L 663536)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

MK-886 (Synonyms: L 663536) 纯度: 99.74%

MK-886 (L 663536) 是一种有效的,细胞可渗透的且具有口服活性的 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。MK-886 也是一种非竞争性 PPARα 拮抗剂,可以诱导细胞凋亡。

MK-886(Synonyms: L 663536)

MK-886 Chemical Structure

CAS No. : 118414-82-7

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥770 In-stock
5 mg ¥700 In-stock
10 mg ¥1200 In-stock
25 mg ¥2300 In-stock
50 mg ¥4100 In-stock
100 mg ¥5600 In-stock
200 mg   询价  
500 mg   询价  

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MK-886 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Cell Cycle/DNA Damage Compound Library
  • GPCR/G Protein Compound Library
  • Immunology/Inflammation Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Orally Active Compound Library
  • Transcription Factor Targeted Library

生物活性

MK-886 (L 663536) is a potent, cell-permeable and orally active FLAP (IC50 of 30 nM) and leukotriene biosynthesis (IC50s of 3 nM and 1.1 μM in intact leukocytes and human whole blood, respectively) inhibitor. MK-886 is also a non-competitive PPARα antagonist and can induce apoptosis[1][2][3].

IC50 & Target

IC50: 30 nM (FLAP)[3]
IC50: 3 nM (Leukotriene biosynthesis in intact leukocytes) and 1.1 μM (Leukotriene biosynthesis in human whole blood)[2]
PPARα[1]

体外研究
(In Vitro)

MK-886 (0.5-2 µM; 15 hours; primary keratinocytes) treatment reduces keratin-1 expression in a culture of mouse primary keratinocytes[1].
Using a transient transfection system in monkey kidney fibroblast CV-1 cells, mouse keratinocyte 308 cells and human lung adenocarcinoma A549 cells, 10 µM MK-886 is able to inhibit Wy-14643 activation of PPARα by ~80%. MK-886 also decreases PPARα activation by fatty acids in the stable transfection system[1].
Although Jurkat cells express all PPAR isoforms, various PPARα and PPARγ agonists are unable to prevent MK-886-induced apoptosis[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: Primary keratinocytes
Concentration: 0.5 µM, 1 µM or 2 µM
Incubation Time: 15 hours
Result: Decreased in keratin-1 expression.

体内研究
(In Vivo)

MK-886 (L 663536; 5 mg/kg; oral administration; male Sprague-Dawley rats) treatment potently inhibits the antigen-induced dyspnea in inbred rats pretreated with methysergide[2].
MK-886 (L 663536) inhibits leukotriene biosynthesis in vivo in a rat pleurisy model (ED50, 0.2 mg/kg p.o.), an inflamed rat paw model (ED50, 0.8 mg/kg), a model of leukotriene excretion in rat bile following antigen provocation[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Sprague-Dawley rats (300-400 g) with antigen-induced dyspnea[1]
Dosage: 5 mg/kg
Administration: Oral administration
Result: Inhibited the antigen-induced dyspnea.

分子量

472.08

Formula

C27H34ClNO2S

CAS 号

118414-82-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 75 mg/mL (158.87 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1183 mL 10.5914 mL 21.1828 mL
5 mM 0.4237 mL 2.1183 mL 4.2366 mL
10 mM 0.2118 mL 1.0591 mL 2.1183 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 0.5% CMC-Na/saline water

    Solubility: 10 mg/mL (21.18 mM); Suspended solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (5.30 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (5.30 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.08 mg/mL (4.41 mM); Clear solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (4.41 mM) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 4.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.41 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.41 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. [1] Kehrer JP et al. Inhibition of peroxisome-proliferator-activated receptor (PPAR)alpha by MK886. Biochem J. 2001 Jun 15.

    [2]. [2] Gillard J et al. 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. 1989 May;67(5):456-64.

    [3]. Mancini JA, et al. 5-Lipoxygenase-activating protein is the target of a novel hybrid of two classes of leukotriene biosynthesis inhibitors. Mol Pharmacol. 1992 Feb;41(2):267-72.

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