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  3. Quiflapon sodium

Quiflapon sodium (Synonyms: MK591)

Cat. No.: HY-50714 Purity: 99.91%
Handling Instructions

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

For research use only. We do not sell to patients.

Quiflapon sodium Chemical Structure

Quiflapon sodium Chemical Structure

CAS No. : 147030-01-1

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10 mM * 1 mL in DMSO USD 177 In-stock
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5 mg USD 132 In-stock
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10 mg USD 210 In-stock
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50 mg USD 900 In-stock
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100 mg USD 1320 In-stock
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Description

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

In Vitro

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].

In Vivo

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].

Molecular Weight

609.15

Formula

C₃₄H₃₄ClN₂NaO₃S

CAS No.

147030-01-1

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+]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (82.08 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.75 mg/mL (4.51 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.75 mg/mL (4.51 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Kinase Assay
[2]

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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[4]

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).

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 99.91%

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Keywords:

QuiflaponMK591MK 591MK-591FLAP5-lipoxygenase-activating protein5-LO activating proteinInhibitorinhibitorinhibit

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Product name:
Quiflapon sodium
Cat. No.:
HY-50714
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