Veliflapon_product_DataBase

Bioactivity

Veliflapon (BAY X 1005; DG-031) is an orally active and selective 5-lipoxygenase activating protein (FLAP) inhibitor[1]. Veliflapon inhibits the synthesis of the leukotrienes B4 and C4[2].

Invitro

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[3].

In Vivo

Veliflapon (BAY X 1005; DG-031; diet; 18.8 mg/kg/day for 16 weeks ) inhibits atherogenesis[4]. 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[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]. Animal Model:

Name

Veliflapon

CAS

128253-31-6

Formula

C23H23NO3

Molar Mass

361.43

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[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.

PeptideDB

Veliflapon

CAS: 128253-31-6 F: C23H23NO3 W: 361.43