Roflumilast

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Cat.No. 6641 - Roflumilast | C17H14Cl2F2N2O3 | CAS No. 162401-32-3
Description: Potent and selective PDE4 inhibitor
Chemical Name: 3-(Cyclopropylmethoxy)-N-(3,5-dichloro-4-pyridinyl)-4-(difluoromethoxy)benzamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

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

M. Wt 403.21
Formula C17H14Cl2F2N2O3
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 162401-32-3
PubChem ID 449193
InChI Key MNDBXUUTURYVHR-UHFFFAOYSA-N
Smiles FC(F)OC(C=C1)=C(OCC2CC2)C=C1C(NC3=C(Cl)C=NC=C3Cl)=O

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

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
ethanol 4.03 10
DMSO 40.32 100

Preparing Stock Solutions

The following data is based on the product molecular weight 403.21. Batch specific molecular weights may vary from batch to batch due to solvent 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

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References

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

Hatzelmann et al (2010) The preclinical pharmacology of roflumilast - 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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