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Quiflapon sodium Sale

(Synonyms: 喹夫拉朋钠,MK-591 sodium) 目录号 : GC37059

Quiflapon sodium (MK591) 是选择性的,特异性的 FLAP 抑制剂。

Quiflapon sodium Chemical Structure

Cas No.:147030-01-1

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Free Sample (0.1-0.5 mg) 待询 待询
10mM (in 1mL DMSO)
¥1,234.00
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5mg
¥921.00
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10mg
¥1,465.00
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50mg
¥6,278.00
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100mg
¥9,207.00
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200mg 待询 待询
500mg 待询 待询

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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

Kinase experiment:

LNCaP cells (appr 3×105) are plated and treated with inhibitors or solvent vehicle for varying periods of time. Then the cells are lysed in lysis buffer containing 0.2% CHAPS detergent plus protease and phosphatase inhibitors, and the enzymatic activity of Akt is measured by a kit following methods supplied by the manufacturer.

Animal experiment:

The Tg2576 transgenic mice expressing human APP with the Swedish mutation (K670N/M671L) are used in these studies. They are genotyped by PCR analysis using tail DNA and kept in a pathogen-free environment, on a 12-hour light/dark cycle and have access to food and water ad libitum. All the experiments presented in this paper are performed with female mice. Starting at 7 months of age, mice are randomized to receive MK-591 (40 mg/kg weight) (n=11) or vehicle (n=9) in their chow diet for 8 months until they are 15 months old. Considering that each mouse eats on average 5 g/day of chow diet and the diet is formulated for 320 mg Quiflapon sodium (MK591) per kg diet, the final dose of the active drug is approximately 40 mg/kg weight/day. During the study, mice in both groups gain weight regularly, and no significant difference in weight is detected between the two groups. No macroscopic effect on the overall general health is observed in the animals receiving the active treatment. Post-mortem examination shows no sign of macroscopic pathology in any of the organs considered (spleen, liver, thymus, ileum).

References:

[1]. Mendis C, et al. Effect of 5-lipoxygenase inhibitor MK591 on early molecular and signaling events induced by staphylococcal enterotoxin B in human peripheral blood mononuclear cells. FEBS J. 2008 Jun;275(12):3088-98.
[2]. Sarveswaran S, et al. MK591, a leukotriene biosynthesis inhibitor, induces apoptosis in prostate cancer cells: synergistic action with LY294002, an inhibitor of phosphatidylinositol 3'-kinase. Cancer Lett. 2010 May 28;291(2):167-76.
[3]. Park MS, et al. 5-Lipoxygenase-activating protein (FLAP) inhibitor MK-0591 prevents aberrant alveolarization in newborn mice exposed to 85% oxygen in a dose- and time-dependent manner. Lung. 2011 Feb;189(1):43-50.
[4]. Chu J, et al. Involvement of 5-lipoxygenase activating protein in the amyloidotic phenotype of an Alzheimer's disease mouse model. J Neuroinflammation. 2012 Jun 14;9:127.

产品描述

Quiflapon sodium (MK591) is a selective and specific 5-Lipoxygenase-activating protein (FLAP) inhibitor.

Quiflapon sodium (MK591) and SB203580 are able to block SEB-induced human PBMC cell proliferation. Quiflapon sodium (MK591) down regulates three genes [for cathepsin L, IL-17 and guanylate binding protein (GBP)-2] that are up regulated by SEB[1]. Quiflapon sodium (MK591) undergoes apoptosis within hours of treatment. Quiflapon sodium (MK591) also induces rapid activation of the stress kinase, c-Jun N-terminal kinase (JNK), which plays an important role in the apoptosis process. Quiflapon sodium (MK591) triggers apoptosis in prostate cancer cells without inhibition of PI3K-Akt, or ERK. Moreover, MK591 and LY294002 (an inhibitor of PI3K) exert synergistic effect in inducing apoptosis in prostate cancer cells[2]. Quiflapon sodium (MK591) influences cAMP response element-binding protein but not Sp1[4].

Hyperoxia groups of mice treated with Quiflapon sodium (MK591) (20, 40 mg/kg) show alveolarization that resembles that of room air controls while untreated hyperoxia groups show definite evidence of aberrant alveolarization but no inflammation[3]. Comparison of the Aβ-immunopositive areas between the placebo and Quiflapon sodium (MK591) (320 mg/kg)-treated group reveals a statistically significant reduction of the amyloid burden in the treated mice. Quiflapon sodium (MK591) also has a significant reduction in brain levels of IL-1β. Mice treated with Quiflapon sodium (MK591) show a statistically significant decrease in the steady-state levels of total CREB and its phosphorylated form at Ser133[4].

[1]. Mendis C, et al. Effect of 5-lipoxygenase inhibitor MK591 on early molecular and signaling events induced by staphylococcal enterotoxin B in human peripheral blood mononuclear cells. FEBS J. 2008 Jun;275(12):3088-98. [2]. Sarveswaran S, et al. MK591, a leukotriene biosynthesis inhibitor, induces apoptosis in prostate cancer cells: synergistic action with LY294002, an inhibitor of phosphatidylinositol 3'-kinase. Cancer Lett. 2010 May 28;291(2):167-76. [3]. Park MS, et al. 5-Lipoxygenase-activating protein (FLAP) inhibitor MK-0591 prevents aberrant alveolarization in newborn mice exposed to 85% oxygen in a dose- and time-dependent manner. Lung. 2011 Feb;189(1):43-50. [4]. Chu J, et al. Involvement of 5-lipoxygenase activating protein in the amyloidotic phenotype of an Alzheimer's disease mouse model. J Neuroinflammation. 2012 Jun 14;9:127.

Chemical Properties

Cas No. 147030-01-1 SDF
别名 喹夫拉朋钠,MK-591 sodium
Canonical SMILES [O-]C(C(C)(C)CC(N1CC2=CC=C(Cl)C=C2)=C(SC(C)(C)C)C3=C1C=CC(OCC4=NC5=CC=CC=C5C=C4)=C3)=O.[Na+]
分子式 C34H34ClN2NaO3S 分子量 609.15
溶解度 DMSO: 50 mg/mL (82.08 mM); Water: < 0.1 mg/mL (insoluble) 储存条件 Store at -20°C
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储备液的保存方式和期限:-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。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.6416 mL 8.2082 mL 16.4163 mL
5 mM 0.3283 mL 1.6416 mL 3.2833 mL
10 mM 0.1642 mL 0.8208 mL 1.6416 mL
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