Roflumilast

Key Product Details

Product Description

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.

Product Specifications for Roflumilast

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for Roflumilast

The following data is based on the product molecular weight 403.21.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.48 mL	12.40 mL	24.80 mL
5 mM	0.50 mL	2.48 mL	4.96 mL
10 mM	0.25 mL	1.24 mL	2.48 mL
50 mM	0.05 mL	0.25 mL	0.50 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Rabe Update on roflumilast, a phosphodiesterase 4 inhibitor for the treatment of chronic obstructive pulmonary disease. Br.J.Pharmacol. 2011 PMID: 21232047
• Hatzelmann The preclinical pharmacology of roflum. - a selective, oral phosphodiesterase 4 inhibitor in development for chronic obstructive pulmonary disease. Pulm.Pharmacol.Ther. 2010 PMID: 20381629

Product Documents for Roflumilast