For research use only. Not for therapeutic Use.
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].
AM679 is a potent, selective inhibitor of FLAP, as demonstrated in an in vitro human FLAP membrane binding assay with IC50 of 2 nM and when assayed as an inhibitor of ex vivo ionophore-challenged mouse and human blood LTB4 synthesis with IC50s of 55 nM and 154 nM, respectively[1].
AM679 is a potent and selective FLAP inhibitor with IC50s of 2.2 nM/0.6 nM/154 nM for FLAP binding/hLA/hWB respectively[2].
AM679 shows potent inhibition of leukotrienes in human blood and in a rodent bronchoalvelolar lavage challenge model[2].
Catalog Number | I000770 |
CAS Number | 1206880-66-1 |
Synonyms | 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 |
Molecular Formula | C40H44N4O5S |
Purity | ≥95% |
InChI | InChI=1S/C40H44N4O5S/c1-25(45)44-29(18-28-10-8-9-11-33(28)44)24-49-30-16-17-34-32(19-30)36(50-39(2,3)4)35(20-40(5,6)38(46)47)43(34)23-26-12-14-27(15-13-26)37-41-21-31(48-7)22-42-37/h8-17,19,21-22,29H,18,20,23-24H2,1-7H3,(H,46,47)/t29-/m0/s1 |
InChIKey | VYXWHVDEWWHDLH-LJAQVGFWSA-N |
SMILES | CC(=O)N1C(CC2=CC=CC=C21)COC3=CC4=C(C=C3)N(C(=C4SC(C)(C)C)CC(C)(C)C(=O)O)CC5=CC=C(C=C5)C6=NC=C(C=N6)OC |
Reference | [1]. Musiyenko, A, 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]. Stock, N, 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 inhib |