| Bioactivity | 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]. | ||||||||||||
| Invitro | 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]. | ||||||||||||
| In Vivo | AM679 shows potent inhibition of leukotrienes in human blood and in a rodent bronchoalvelolar lavage challenge model[2]. | ||||||||||||
| Name | AM679 | ||||||||||||
| CAS | 1206880-66-1 | ||||||||||||
| Formula | C40H44N4O5S | ||||||||||||
| Molar Mass | 692.87 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| 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 |