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CAS No. : 128253-31-6
MCE 国际站:Veliflapon
产品活性:Veliflapon (BAY X 1005; DG-031) 是一种具有口服活性的,选择性的 5-脂氧合酶激活蛋白 (FLAP) 抑制剂。Veliflapon 也是白三烯 B4 和 C4 合成的抑制剂。
研究领域:Immunology/Inflammation | GPCR/G Protein
作用靶点:FLAP | Leukotriene Receptor
In Vitro: Veliflapon (BAY X 1005; DG-031) effectively inhibits the synthesis of LTB4 in A23187-stimulated leukocytes from rats, mice and humans (IC50s of 0.026, 0.039 and 0.22 μM, respectively) as well as the formation of LTC4 (IC50 of 0.021 μM) in mouse peritoneal macrophages stimulated with opsonized zymosan.
In Vivo: Veliflapon (BAY X 1005; DG-031; diet; 18.8 mg/kg/day for 16 weeks ) inhibits atherogenesis.
Veliflapon after topical (18 μg/ear) and oral (48.7 mg/kg) administration has antiedematous effects in the arachidonic acid-induced mouse ear inflammation test.
Veliflapon is potent (11.8 and 6.7 mg/kg p.o. at 1 and 5 hours, respectively) and has a long duration of action (ED40 of 16 hours, 70 mg/kg p.o.) in the rat whole blood ex vivo leukotriene B4 inhibition assay.
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