Description
MK-0591 is a selective and specific inhibitor of 5-Lipoxygenase-activating protein (FLAP).
Product Overview
MK-0591, an analog of MK-886 is a potent and orally active leukotriene biosynthesis inhibitor with an IC50 value of 600 ng/ml. MK-0591 (250 mg) nearly completely inhibited systemic leukotriene synthesis (>90%) in whole blood or in patients with active disease, and induced LTB4 synthesis in the target tissue of inflammation. MK-0591 plays as a potential agent for the treatment of asthma and inflammatory bowel disease. MK-0591 specific interacted with 5-lipoxygenase, a membrane protein activating protein FLAP, which is essential for LT synthesis in inflammatory cells. MK-0591 inhibited 96% production of LTB4 in whole blood and 91% that from BAL cells. By contrast, MK-0591 had no effect on airway hyper-responsiveness, ozone-induced bronchoconstriction, or influx of neutrophils into BAL.
Synonyms
Quiflapon; MK0591; MK 0591
Molecular Formula
C34H35ClN2O3S
Chemical Name
3-[3-tert-butylsulfanyl-1-[(4-chlorophenyl)methyl]-5-(quinolin-2-ylmethoxy)indol-2-yl]-2,2-dimethylpropanoic acid
Solubility
Soluble in DMSO
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request