AM-679
- Product Name
- AM-679
- CAS No.
- 1206880-66-1
- Chemical Name
- AM-679
- Synonyms
- AM-679;AM-679;AM 679;(2-iodophenyl)(1-pentyl-1H-indol-3-yl)Me-thanon;(S)-3-(5-((1-acetylindolin-2-yl)methoxy)-3-(tert-Butylthio)-1-(4-(5-methoxypyrimidin-2-yl)benzyl)-1H-indol-2-yl)-2,2-dimethylpropanoic acid;3-{5-((S)-N-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;1H-Indole-2-propanoic acid, 5-[[(2S)-1-acetyl-2,3-dihydro-1H-indol-2-yl]methoxy]-3-[(1,1-dimethylethyl)thio]-1-[[4-(5-methoxy-2-pyrimidinyl)phenyl]methyl]-α,α-dimethyl-;5-[[(2S)-1-Acetyl-2,3-dihydro-1H-indol-2-yl]methoxy]-3-[(1,1-dimethylethyl)thio]-1-[[4-(5-methoxy-2-pyrimidinyl)phenyl]methyl]-alpha,alpha-dimethyl-1H-indole-2-propanoic acid
- CBNumber
- CB92551767
- Molecular Formula
- C40H44N4O5S
- Formula Weight
- 692.87
- MOL File
- 1206880-66-1.mol
AM-679 Property
- Boiling point:
- 837.1±65.0 °C(Predicted)
- Density
- 1.23±0.1 g/cm3(Predicted)
- solubility
- Soluble in DMSO
- form
- crystalline solid
- pka
- 4.69±0.10(Predicted)
- color
- Off-white to pink
N-Bromosuccinimide Price
- Product number
- A3169
- Product name
- AM679
- Packaging
- 5mg
- Price
- $305
- Updated
- 2021/12/16
- Product number
- CS-0935
- Product name
- AM679
- Purity
- 99.72%
- Packaging
- 5mg
- Price
- $312
- Updated
- 2021/12/16
- Product number
- A3169
- Product name
- AM679
- Packaging
- 10mg
- Price
- $394
- Updated
- 2021/12/16
- Product number
- CS-0935
- Product name
- AM679
- Purity
- 99.72%
- Packaging
- 10mg
- Price
- $403
- Updated
- 2021/12/16
- Product number
- A3169
- Product name
- AM679
- Packaging
- 50mg
- Price
- $1062
- Updated
- 2021/12/16
AM-679 Chemical Properties,Usage,Production
Uses
AM679 is a potent, selective 5-lipoxygenase-activating protein (FLAP) inhibitor with an IC50 of 2 nM in a human FLAP membrane binding assay. AM679 markedly reduces the respiratory syncytial virus-driven ocular pathology as well as the synthesis of cysteinyl leukotrienes (CysLTs) in the eye[1].
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].
in vivo
AM679 shows potent inhibition of leukotrienes in human blood and in a rodent bronchoalvelolar lavage challenge model[2].
target
FLAP
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.
AM-679 Preparation Products And Raw materials
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