1206880-66-1 Usage
Biological Activity
am679 is a topically applied and potent 5-lipoxygenase-activating protein (flap) inhibitor with an ic50 value of 2.2 nm [1] [2].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 [2].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 [2].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 [1].
references
[1]. alla musiyenko, lucia correa, nicholas stock, et al. a novel 5-lipoxygenase-activating protein inhibitor, am679, reduces inflammation in the respiratory syncytial virus-infected mouse eye. clinical and vaccine immunology, 2009, 16(11):1654-1659.[2]. nicholas stock, christopher baccei, gretchen bain, et al. 5-lipoxygenase-activating protein inhibitors. part 2: 3-{5-((s)-1-acetyl-2,3-dihydro-1h-indol-2-ylmethoxy)-3-tert-butylsulfanyl-1-[4-(5-methoxy-pyrimidin-2-yl)-benzyl]-1h-indol-2-yl}-2,2-dimethyl-propionic acid (am679)—a potent flap inhibitor. bioorganic & medicinal chemistry letters, 2010, 20:213-217.
Check Digit Verification of cas no
The CAS Registry Mumber 1206880-66-1 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,2,0,6,8,8 and 0 respectively; the second part has 2 digits, 6 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 1206880-66:
(9*1)+(8*2)+(7*0)+(6*6)+(5*8)+(4*8)+(3*0)+(2*6)+(1*6)=151
151 % 10 = 1
So 1206880-66-1 is a valid CAS Registry Number.
1206880-66-1Relevant articles and documents
5-Lipoxygenase-activating protein inhibitors. Part 2: 3-{5-((S)-1-Acetyl-2,3-dihydro-1H-indol-2-ylmethoxy)-3-tert-butylsulfanyl-1-[4-(5-methoxy-pyrimidin-2-yl)-benzyl]-1H-indol-2-yl}-2,2-dimethyl-propionic acid (AM679)-A potent FLAP inhibitor
Stock, Nicholas,Baccei, Christopher,Bain, Gretchen,Broadhead, Alex,Chapman, Charles,Darlington, Janice,King, Christopher,Lee, Catherine,Li, Yiwei,Lorrain, Daniel S.,Prodanovich, Pat,Rong, Haojing,Santini, Angelina,Zunic, Jasmine,Evans, Jilly F.,Hutchinson, John H.,Prasit, Peppi
scheme or table, p. 213 - 217 (2010/04/24)
A series of potent 5-lipoxygenase-activating protein (FLAP) inhibitors are herein described. SAR studies focused on the discovery of novel alicyclic moieties appended to an indole core to optimize potency, physical properties and off-target activities. Subsequent SAR on the N-benzyl substituent of the indole led to the discovery of compound 39 (AM679) which showed potent inhibition of leukotrienes in human blood and in a rodent bronchoalvelolar lavage (BAL) challenge model.
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