Quiflapon

• CAT Number: I001412
• CAS Number: 136668-42-3
• Molecular Formula: C34H35ClN2O3S
• Molecular Weight: 587.17
• Purity: 98%
• Target: FLAP
• Solubility: 10 mM in DMSO
• Storage: Store at -20°C
• Related CAS: 147030-01-1 (sodium)
• IC50: 1.6 nM
• IUPAC Name: 3-[3-tert-butylsulfanyl-1-[(4-chlorophenyl)methyl]-5-(quinolin-2-ylmethoxy)indol-2-yl]-2,2-dimethylpropanoic acid
• InChI: InChI=1S/C34H35ClN2O3S/c1-33(2,3)41-31-27-18-26(40-21-25-15-12-23-8-6-7-9-28(23)36-25)16-17-29(27)37(20-22-10-13-24(35)14-11-22)30(31)19-34(4,5)32(38)39/h6-18H,19-21H2,1-5H3,(H,38,39)
• InChIKey: NZOONKHCNQFYCI-UHFFFAOYSA-N
• SMILES: CC(C)(C)SC1=C(N(C2=C1C=C(C=C2)OCC3=NC4=CC=CC=C4C=C3)CC5=CC=C(C=C5)Cl)CC(C)(C)C(=O)O

Quiflapon (Cat No.:I001412) is a highly selective and specific inhibitor of 5-lipoxygenase-activating protein (FLAP) with an IC50 value of 1.6nM. It is also a potent inhibitor of leukotriene biosynthesis, with IC50 values of 3.1nM and 6.1nM in intact human and induced rat polymorphonuclear leukocyte PMNLs, respectively. Quiflapon can induce apoptosis, a process of programmed cell death.

Reference

[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.