1. Immunology/Inflammation
    Apoptosis
  2. FLAP
    Apoptosis
  3. Quiflapon

Quiflapon (Synonyms: MK-591)

Cat. No.: HY-10037 Purity: 99.44%
Handling Instructions

Quiflapon (MK-591) est un inhibiteur sélectif et spécifique de la protéine d'activation de la 5-lipoxygénase (FLAP) avec un IC50 de 1,6 nM dans un test de liaison FLAP. Quiflapon est également un inhibiteur de la biosynthèse des leucotriènes (LT) puissant et oralement actif, présente des valeurs IC50 de 3,1 et 6,1 nM chez l'homme intact et suscité. PMNL de rat, respectivement. Quiflapon induit l'apoptose cellulaire.

Quiflapon (MK-591) is a selective and specific 5-lipoxygenase-activating protein (FLAP) inhibitor with an IC50 of 1.6 nM in a FLAP binding assay. Quiflapon is also a potent and orally active Leukotriene biosynthesis (LT) inhibitor, shows IC50 values of 3.1 and 6.1 nM in intact human and elicited rat PMNLs, respectively. Quiflapon induces cell apoptosis.

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

Quiflapon Chemical Structure

Quiflapon Chemical Structure

CAS No. : 136668-42-3

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Description

Quiflapon (MK-591) is a selective and specific 5-lipoxygenase-activating protein (FLAP) inhibitor with an IC50 of 1.6 nM in a FLAP binding assay. Quiflapon is also a potent and orally active Leukotriene biosynthesis (LT) inhibitor, shows IC50 values of 3.1 and 6.1 nM in intact human and elicited rat PMNLs, respectively. Quiflapon induces cell apoptosis[1][2].

IC50 & Target

IC50: 1.6 nM (FLAP)[1].

In Vitro

Quiflapon is a potent inhibitor of leukotriene (LT) biosynthesis in intact human and elicited rat polymorphonuclear leukocytes (PMNLs) (IC50 values 3.1 and 6.1 nM, respectively) and in human, squirrel monkey, and rat whole blood (IC50 values 510, 69, and 9 nM, respectively). Quiflapon has no effect on rat 5-lipoxygenase. Quiflapon has a high affinity for 5-lipoxygenase activating protein (FLAP) as evidenced by an IC50 value of 1.6 nM in a FLAP binding assay and inhibition of the photoaffinity labelling of FLAP by two different photoaffinity ligands. Inhibition of activation of 5-lipoxygenase was shown through inhibition of the translocation of the enzyme from the cytosol to the membrane in human PMNLs[1].

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

In Vivo

Quiflapon is a potent inhibitor of LT biosynthesis in vivo, first, following ex vivo challenge of blood obtained from treated rats and squirrel monkeys, second, in a rat pleurisy model, and, third, as monitored by inhibition of the urinary excretion of LTE4 in antigen-challenged allergic sheep. Inhibition of antigen-induced bronchoconstriction by Quiflapon is observed in inbred rats pretreated with methysergide, Ascaris-challenged squirrel monkeys, and Ascaris-challenged sheep (early and late phase response) [1]. Pups were treated with either vehicle or Quiflapon 10, 20, or 40 mg/kg subcutaneously daily for days 1-4, 5-9, or 10-14. On day 14, the lungs were inflated, fixed, and stained for histopathological and morphometric analyses. Hyperoxia groups treated with Quiflapon untreated hyperoxia groups showed definite evidence of aberrant alveolarization but no inflammation[2].

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

Molecular Weight

587.17

Formula

C₃₄H₃₅ClN₂O₃S

CAS No.

136668-42-3

SMILES

O=C(O)C(C)(C)CC1=C(SC(C)(C)C)C2=C(C=CC(OCC3=NC4=CC=CC=C4C=C3)=C2)N1CC5=CC=C(Cl)C=C5

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 (85.15 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7031 mL 8.5154 mL 17.0308 mL
5 mM 0.3406 mL 1.7031 mL 3.4062 mL
10 mM 0.1703 mL 0.8515 mL 1.7031 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: 2.5 mg/mL (4.26 mM); Suspended solution; Need ultrasonic and warming

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (4.26 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

QuiflaponMK-591MK591MK 591FLAPApoptosis5-lipoxygenase-activating protein5-LO activating proteinInhibitorinhibitorinhibit

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