| Description | Veliflapon is an orally active and selective inhibitor of 5-lipoxygenase activating protein (FLAP). Veliflapon inhibits the synthesis of the leukotrienes B4 and C4. |
| In vitro | Veliflapon inhibits the synthesis of LTB4 in A23187-stimulated leukocytes from rats, mice and humans with IC50s of 0.026, 0.039 and 0.22 μM, respectively as well as the formation of LTC4 with IC50 of 0.021 μM in mouse peritoneal macrophages stimulated with opsonized zymosan[3]. |
| In vivo | Atherogenesis inhibited by Veliflapon (DG-031; diet; 18.8 mg/kg/day for 16 weeks ). In the arachidonic acid-induced mouse ear inflammation test,Veliflapon after topical (18 μg/ear) and oral (48.7 mg/kg) administration has antiedematous effects [4]. 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[4]. |
| Synonyms | DG-031, BAY X 1005 |
| molecular weight | 361.43 |
| Molecular formula | C23H23NO3 |
| CAS | 128253-31-6 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| References | 1. Hatzelmann A, et al. Mode of action of the leukotriene synthesis (FLAP) inhibitor BAY X 1005: implications for biological regulation of 5-lipoxygenase. Agents Actions. 1994 Nov;43(1-2):64-8. 2. Müller-Peddinghaus R, et al. BAY X1005, a new inhibitor of leukotriene synthesis: in vivo inflammation pharmacology and pharmacokinetics. J Pharmacol Exp Ther. 1993 Oct;267(1):51-7. 3. 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. 4. Jawień J, et al. BAY x 1005 attenuates atherosclerosis in apoE/LDLR - double knockout mice. J Physiol Pharmacol. 2007 Sep;58(3):583-8. |