Quiflapon sodium |
| Catalog No.GC37059 |
Quiflapon sodium (MK-591 sodium) is a selective and specific 5-Lipoxygenase-activating protein (FLAP) inhibitor.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 147030-01-1
Sample solution is provided at 25 µL, 10mM.
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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.
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. | |
| Cas No. | 147030-01-1 | SDF | |
| 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+] | ||
| Formula | C34H34ClN2NaO3S | M.Wt | 609.15 |
| Solubility | DMSO: 50 mg/mL (82.08 mM); Water: < 0.1 mg/mL (insoluble) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 19 reference(s) in Google Scholar.)
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