MK591
This product is for research use only, not for human use. We do not sell to patients.
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Size | Price | Stock |
---|---|---|
250mg | $1450 | Check With Us |
500mg | $2280 | Check With Us |
1g | $3420 | Check With Us |
Cat #: V4319 CAS #: 136668-42-3 Purity ≥ 98%
Description: Quiflapon (formerly known as L-686,70 and MK591 free acid) is a novel, potent, selective and specific 5-Lipoxygenase-activating protein (FLAP) inhibitor with an IC50 value of 1.6 nM in a FLAP binding assay.
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Molecular Weight (MW) | 587.17 |
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Molecular Formula | C34H35ClN2O3S |
CAS No. | 136668-42-3 |
Storage | -20℃ for 3 years in powder formr |
-80℃ for 2 years in solvent | |
SMILES Code | O=C(O)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 |
Synonyms | MK 0591; MK-0591; MK0591; L 686708; L-686708; L686708; L-686,708; L 686,708; L686,708; MK 591; MK591; MK-591; Quiflapon; Quiflapon sodium; |
Protocol | 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. |
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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. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
Solvent volume to be added | Mass (the weight of a compound) | |||
---|---|---|---|---|
Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
1mM | 1.7031 mL | 8.5154 mL | 17.0308 mL | 34.0617 mL |
5mM | 0.3406 mL | 1.7031 mL | 3.4062 mL | 6.8123 mL |
10mM | 0.1703 mL | 0.8515 mL | 1.7031 mL | 3.4062 mL |
20mM | 0.0852 mL | 0.4258 mL | 0.8515 mL | 1.7031 mL |
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Step Two: Enter the in vivo formulation
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%ddH2O
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Method for preparing DMSO master liquid:
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Method for preparing in vivo formulation:
Take
µL
DMSO master liquid, next add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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