(S)-Veliflapon ((S)-BAY X 1005) is an orally active inhibitor of leukotriene biosynthesis and 5-lipoxygenase activating protein (FLAP). (S)-Veliflapon inhibits the formation of leukotriene B4 (LTB4) in rat, mouse and human leukocytes with IC50 values of 0.026 µM, 0.039 µM and 0.22 µM respectively. (S)-Veliflapon showes enantioselectivity in human whole blood[1][2][3].
(S)-Veliflapon 以剂量依赖性方式减少了人全血中白三烯 B4 (LTB4) 的合成[1]。
[1]. Fruchtmann R, et al. In vitro pharmacology of BAY X1005, a new inhibitor of leukotriene synthesis. Agents Actions. 1993 Mar;38(3-4):188-95.
[2]. Hermann, David J., et al. Dosing schedules of leukotriene synthesis inhibitors for human therapy. World Intellectual Property Organization. WO2009002746.
[3]. Helgadottir, et al. Polymorphisms in the susceptibility genes for myocardial infarction, stroke, and peripheral artery occlusive disease and their use in risk assessment and proplaxis therapy. United States. US20070280917.