2016年6月8日星期三

AM679|cas 1206880-66-1|DC Chemicals

AM679|cas 1206880-66-1|DC Chemicals

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.

Product Name: AM679|Cat No: DC9447|Cas: 1206880-66-1|Molecule Formular: C40H44N4O5S|Molecule Weight: 692.8661|Other names: AM679

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).

For research only, not for human use!

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