2. Immunology/Inflammation
    Apoptosis
  3. FLAP
    Apoptosis
  4. Quiflapon sodium

Quiflapon sodium  (Synonyms: MK-591 sodium)

Cat. No.: HY-50714 Purity: 99.64%
COA Handling Instructions

Quiflapon sodium (MK-591 sodium) is a selective and specific 5-Lipoxygenase-activating protein (FLAP) inhibitor. Quiflapon sodium is an orally active Leukotriene biosynthesis inhibitor. Induces apoptosis.

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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Solution
10 mM * 1 mL in DMSO USD 177 In-stock
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10 mM * 1 mL
ready for reconstitution
 USD 177 In-stock
Solid
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10 mg USD 210 In-stock
50 mg USD 900 In-stock
100 mg USD 1320 In-stock
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Description

Quiflapon sodium (MK-591 sodium) is a selective and specific 5-Lipoxygenase-activating protein (FLAP) inhibitor. Quiflapon sodium is an orally active Leukotriene biosynthesis inhibitor. Induces apoptosis.

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 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 triggers apoptosis in prostate cancer cells without inhibition of PI3K-Akt, or ERK. Moreover, Quiflapon sodium and LY294002 exert synergistic effect in inducing apoptosis in prostate cancer cells[2]. Quiflapon sodium (MK591) influences cAMP response element-binding protein but not Sp1[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 also has a significant reduction in brain levels of IL-1β. Mice treated with Quiflapon sodium show a statistically significant decrease in the steady-state levels of total CREB and its phosphorylated form at Ser133[4].

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

609.15

Appearance

Solid

Formula

C34H34ClN2NaO3S
CAS No.
SMILES

ClC(C=C1)=CC=C1CN2C(CC(C)(C(O[Na])=O)C)=C(SC(C)(C)C)C3=C2C=CC(OCC4=NC5=CC=CC=C5C=C4)=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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 available by MCE.
Purity & Documentation
References
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 Quiflapon sodium (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 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
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

Quiflapon147030-01-1MK-591MK591MK 591FLAPApoptosis5-lipoxygenase-activating protein5-LO activating proteinInhibitorinhibitorinhibit

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