Roflumilast

Biological Activity

Roflumilast is a potent and selective PDE4 inhibitor (IC₅₀ values are 0.2 to 4.3 nM for various splice variants of PDE4). Exhibits > 1000-fold selectivity for PDE4 over other PDE family members. Demonstrates effects on functioning of neutrophils, CD4⁺ and CD8⁺ T-cells, endothelial, epithelial and smooth muscle cells, as well as fibroblasts, in vitro. Attenuates lung inflammation, mucociliary malfunction, lung fibrosis, oxidative stress, pulmonary vascular remodeling and pulmonary hypertension in animal models of COPD disease mechanisms.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. Update on roflumilast, a phosphodiesterase 4 inhibitor for the treatment of chronic obstructive pulmonary disease.
   Rabe
   Br.J.Pharmacol., 2011;163:53
2. The preclinical pharmacology of roflum. - a selective, oral phosphodiesterase 4 inhibitor in development for chronic obstructive pulmonary disease.
   Hatzelmann et al.
   Pulm.Pharmacol.Ther., 2010;23:235

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