| Name | Quiflapon |
| Description | Quiflapon (MK-591) causes cell apoptosis. Quiflapon is a selective and specific 5-lipoxygenase-activating protein (FLAP) inhibitor (IC50: 1.6 nM in a FLAP binding assay) and is also an effective and orally active Leukotriene biosynthesis (LT) inhibitor (IC50: 3.1 and 6.1 nM in intact human and elicited rat PMNLs, respectively). |
| In vitro | Quiflapon is an effective inhibitor of leukotriene (LT) biosynthesis in the human, squirrel monkey, and rat whole blood (IC50: 510, 69, and 9 nM, respectively). 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 labeling of FLAP by two different photoaffinity ligands. However, Quiflapon has no effect on rat 5-lipoxygenase. The 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 | Pups were treated with either vehicle or Quiflapon(10, 20, or 40 mg/kg; daily for days 1-4, 5-9, or 10-14) subcutaneously. On day 14, the lungs were inflated, fixed, and stained for histopathological and morphometric analyses. 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]. Hyperoxia groups treated with Quiflapon untreated hyperoxia groups displayed definite evidence of aberrant alveolarization but no inflammation[2]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : ≥ 50 mg/mL (85.15 mM)
H2O : < 0.1 mg/mL (insoluble)
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| Keywords | MK591 | Quiflapon | FLAP | inhibit | 5-LO activating protein | MK 591 | Inhibitor | Apoptosis |
| Inhibitors Related | Stavudine | 5-Fluorouracil | Acetylcysteine | Myricetin | Sodium 4-phenylbutyrate | L-Ascorbic acid | Dextran sulfate sodium salt (MW 4500-5500) | Metronidazole | Sorafenib | Tributyrin |
| Related Compound Libraries | Apoptosis Compound Library | Bioactive Compound Library | ReFRAME Related Library | Inhibitor Library | NO PAINS Compound Library | Orally Active Compound Library | Bioactive Compounds Library Max | Human Metabolite Library |
United States
