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AM679

CAS：1206880-66-1

产品活性：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. IC50 value: 2.2 nM/0.6 nM/154 nM(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 10 uM) and no CYP3A4 induction. AM679 has an excellent hWB IC50 potency of 154 nM. 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 (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).

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品牌介绍：
☆ TargetMol品牌专业提供各领域信号通路小分子抑制剂、拮抗剂、天然产物、药物筛选化合物。
☆ 产品适应在癌症、免疫学、心血管系统、呼吸、神经科学等多项科学领域的研发使用，超过660万种小分子化合物。
☆ 提供20000多个小分子抑制剂、天然产物和200多个化合物库。
☆ 配备完善的化学合成和生物实验室，可分别提供高品质小分子抑制剂和药物筛选技术服务。
☆ 每批产品都有严格的NMR和HPLC技术检测，以保证产品高纯度高质量。

原创作者：上海陶术生物科技有限公司