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AM679
Cat No.
CEI-1210
Description
AM679 is a selective inhibitor of 5-Lipoxygenase-activating protein (FLAP).
Product Overview
AM679 is a topically applied and potent 5-lipoxygenase-activating protein (FLAP) inhibitor with an IC50 value of 2.2 nM. FLAP and 5-lipoxygenase (5-LO) together convert membrane-derived arachidonic acid to the pro-inflammatory mediator leukotriene epoxide LTA4.LTA4 is hence rapidly converted into either LTB4 by LTA4 hydrolase or LTC4 by LTC4 synthase. Incubation with AM679 for an extended time period (5 h) increased the potency of human blood against LTB4 production with an IC50 value of 53 nM. This time-dependent increase also happened with an IC50 value of 9 nM in rat blood incubated with AM679 for 4 h. Cysteinyl leukotrienes (CysLTs) are known as promoters of inflammation and allergy. Mouse eye infected by RSV began to show increased ocular CysLTs 4 days after infection. AM679 decreased the peak 6-to 8-day of ocular CysLTs by more than 90%. By day 10, concentrations of CysLT for both AM679-treated mouse eyes and control had almost returned to the baseline. A strong correlation between RSV and IL-4 mRNA had been found for human allergic conjunctivitis. 6 days after RSV infection, IL-4 mRNA concentrations were significantly elevated in RSV-infected mouse eyes. Around 14 days, IL-4 mRNA concentrations were hence gradually decreased to near baseline. AM679 could inhibit more than 80% of the IL-4 increase resulted from RSV infection.
CAS No.
1206880-66-1
Molecular Weight
692.87
Purity
0.98
Storage
Store at -20°C
Synonyms
AM-679; AM 679
Targets
FLAP
Molecular Formula
C40H44N4O5S
Chemical Name
3-[5-[[(2S)-1-acetyl-2,3-dihydroindol-2-yl]methoxy]-3-tert-butylsulfanyl-1-[[4-(5-methoxypyrimidin-2-yl)phenyl]methyl]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
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