AM679, inhibitor

AM679

Cat. Num. AAA5754506

• Purity: 98.00%
• Synonyms: AM679; inhibitor

• Purity/Purification: 98.00%
• Form/Format: Solid. Powder

• Solubility: DMSO: 100mg/mL (144.33mM); H2O: <0.1mg/mL (insoluble); (<1mg/ml refers to the product slightly soluble or insoluble)
• Formula: C40H44N4O5S
• SMILES: O=C(C)N1C2=CC=CC=C2C[C@H]1COC3=CC=C(N(CC4=CC=C(C5=NC=C(OC)C=N5)C=C4)C(CC(C)(C(O)=O)C)=C6SC(C)(C)C)C6=C3
• CAS Number: 1206880-66-1
• Target & IC50: Others
• Preparation and Storage: Store at -20 degree C for 3 years powder; -80 degree C for 2 years in solvent

Structure

Related Product Information for AM679, inhibitor

AM679 is a potent and selective FLAP inhibitor with IC50s of 2.2nM/0.6nM/154nM for FLAP binding/hLA/hWB respectively. IC50 value: 2.2nM/0.6nM/154nM(FLAP binding/hLA/hWB) [1] AM679 showed an improved CYP inhibition profile (IC50 3A4 = 16.7 lM, 2C9 = 3.7 lM, 2D6 >30 lM), no time dependent inhibition against CYP3A4 (0.003 min-1 vs 0.057 min-1 for troleandomycin control 10uM) and no CYP3A4 induction. AM679 has an excellent hWB IC50 potency of 154nM. Target: FLAP in vitro: AM679 showed excellent in vitro inhibition against FLAP. in vivo: AM679 was profiled in a rodent bronchoalveolar lavage (BAL) model to measure its ability to inhibit production of leukotrienes in vivo. 16 Oral administration of 39 (10mg/kg as the sodium carboxylate salt) 4 h prior to ionophore challenge reduced LTB4 and CysLT levels in the rodent lung lavage fluid by 98% and 87%, respectively, with corresponding average rodent plasma levels of 605nM (3 h post dose, rat blood LTB4 IC50 = 125nM).

References

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
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
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.
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.