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Quiflapon

Catalog No. T16087 CAS 136668-42-3

Synonyms: MK-591

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).

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Quiflapon, CAS 136668-42-3

Pack Size	Availability	Price/USD
1 mg	In stock	$ 53.00
2 mg	In stock	$ 76.00
5 mg	In stock	$ 101.00
10 mg	In stock	$ 147.00
25 mg	In stock	$ 337.00
50 mg	In stock	$ 490.00
100 mg	In stock	$ 728.00
1 mL * 10 mM (in DMSO)	In stock	$ 157.00

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Purity: 98.88%

Biological Description

Chemical Properties

Storage & Solubility Information

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).
Targets&IC50	FLAP:1.6 nM
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].

Synonyms	MK-591
Molecular Weight	587.17
Formula	C34H35ClN2O3S
CAS No.	136668-42-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: ≥ 50 mg/mL (85.15 mM)

H2O: < 0.1 mg/mL (insoluble)

References and Literature

1. Brideau C, et al. Pharmacology of MK-0591 (3-[1-(4-chlorobenzyl)-3-(t-butylthio)-5-(quinolin-2-yl-methoxy)- indol-2-yl]-2,2-dimethyl propanoic acid), a potent, orally active leukotriene biosynthesis inhibitor. Can J Physiol Pharmacol. 1992 Jun;70(6):799-807. 2. Park MS, et al. 5-Lipoxygenase-activating protein (FLAP) inhibitor MK-0591 prevents aberrant alveolarization in newborn mice exposed to 85% oxygen in a dose- and time-dependent manner. Lung. 2011 Feb;189(1):43-50.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Orally Active Compound Library Apoptosis Compound Library Bioactive Compounds Library Max Immunology/Inflammation Compound Library NO PAINS Compound Library ReFRAME Related Library Bioactive Compound Library Human Metabolite Library

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Keywords

Quiflapon 136668-42-3 Apoptosis Immunology/Inflammation FLAP MK591 inhibit 5-LO activating protein MK 591 Inhibitor MK-591 inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.