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Biological Activity for Roflumilast
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.
Compound Libraries for Roflumilast
Technical Data for Roflumilast
|Storage||Store at +4°C|
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.
Solubility Data for Roflumilast
|Solvent||Max Conc. mg/mL||Max Conc. mM|
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 will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.48 mL||12.4 mL||24.8 mL|
|5 mM||0.5 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||0.5 mL|
References for Roflumilast
References are publications that support the biological activity of the product.
Hatzelmann et al (2010) The preclinical pharmacology of roflum. - a selective, oral phosphodiesterase 4 inhibitor in development for chronic obstructive pulmonary disease. Pulm.Pharmacol.Ther. 23 235 PMID: 20381629
Rabe (2011) Update on roflumilast, a phosphodiesterase 4 inhibitor for the treatment of chronic obstructive pulmonary disease. Br.J.Pharmacol. 163 53 PMID: 21232047
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Citations for Roflumilast
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Literature in this Area
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