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| Cas No.: | 1206880-66-1 |
| Synonyms: | AM-679;AM 679 |
| 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 |
| Formula: | C40H44N4O5S |
| M.Wt: | 692.8661 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | 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. in vitro: AM679 showed excellent in vitro inhibition against FLAP. AM679 has an excellent hWB IC50 potency of 154 nM. 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 10 uM) and no CYP3A4 induction. 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 (10 mg/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 605 nM (3 h post dose, rat blood LTB4 IC50 = 125 nM). |