1. Immunology/Inflammation
  2. FLAP
  3. MK591 free acid

MK591 free acid (Synonyms: Quiflapon)

Cat. No.: HY-10037 Purity: 99.82%
Handling Instructions

MK591 (free acid) is a selective and specific 5-Lipoxygenase-activating protein (FLAP) inhibitor with an IC50 value of 1.6 nM in a FLAP binding assay.

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

MK591 free acid Chemical Structure

MK591 free acid Chemical Structure

CAS No. : 136668-42-3

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10 mM * 1 mL in DMSO USD 202 In-stock
Estimated Time of Arrival: December 31
5 mg USD 156 In-stock
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10 mg USD 210 In-stock
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50 mg USD 931 In-stock
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100 mg USD 1440 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

MK591 (free acid) is a selective and specific 5-Lipoxygenase-activating protein (FLAP) inhibitor with an IC50 value of 1.6 nM in a FLAP binding assay.

IC50 & Target

IC50 value: 1.6 nM (FLAP)[1].

In Vitro

MK591 (free acid) 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). MK591 (free acid) has no effect on rat 5-lipoxygenase. MK591 (free acid) 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].

In Vivo

MK591 (free acid) 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 MK591 (free acid) 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 MK591 (free acid) 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 MK-0591 (free acid) untreated hyperoxia groups showed definite evidence of aberrant alveolarization but no inflammation[2].

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:

MK591QuiflaponMK 591MK-591FLAP5-lipoxygenase-activating protein5-LO activating proteinInhibitorinhibitorinhibit

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MK591 free acid
Cat. No.:
HY-10037
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