Roflumilast N-oxide

Roflumilast N-oxide is an inhibitor of phosphodiesterase 4 (PDE4; IC₅₀ = 2 nM) and an active metabolite of the PDE4 inhibitor roflumilast (Item No. 15141).¹ It is selective for PDE4 over PDE1-3 and PDE5 (IC₅₀s = >10,000 nM for all). It reduces TNF-α-induced ICAM-1 and eotaxin levels when used in combination with prostaglandin E₂ (PGE₂; Item No. 14010) in GM06114 human fetal lung fibroblasts (IC₅₀s = 0.9 and 0.5 nM, respectively).² It also reduces bFGF-induced and IL-1β augmented proliferation in the same cells. Roflumilast N-oxide (2 nM) reverses cigarette smoke extract-induced reductions in ciliary beat frequency in isolated human bronchial epithelial cells.³ Roflumilast N-oxide also increases plasma glucagon-like peptide 1 (GLP-1) levels in a glucose challenge in diabetic db/db mice when administered at a dose of 10 mg/kg, as well as prevents increases in blood glucose in db/db mice at 3 mg/kg per day.⁴

WARNING This product is not for human or veterinary use.

1. Hatzelmann, A., and Schudt, C. Anti-inflammatory and immunomodulatory potential of the novel PDE4 inhibitor roflumilast in vitro. J. Pharmacol. Exp. Ther. 297(1), 267-279 (2001).

2. Sabatini, F., Petecchia, L., Boero, S., et al. A phosphodiesterase 4 inhibitor, roflumilast N-oxide, inhibits human lung fibroblast functions in vitro. Pulm. Pharmacol. Ther. 23(4), 283-291 (2010).

3. Milara, J., Armengot, M., Bañuls, P., et al. Roflumilast N-oxide, a PDE4 inhibitor, improves cilia motility and ciliated human bronchial epithelial cells compromised by cigarette smoke in vitro. Br. J. Pharmacol. 166(8), 2243-2262 (2012).

4. Vollert, S., Kaessner, N., Heuser, A., et al. The glucose-lowering effects of the PDE4 inhibitors roflumilast and roflumilast-N-oxide in db/db mice. Diabetologia 55(10), 2779-2788 (2012).