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Roflumilast

Cat. No. 6641 Submit a Review Datasheet / COA / SDS
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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 (1)
Biological Activity Technical Data Solubility Calculators Datasheets References

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

Roflumilast is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen FDA-Approved Drugs. Find out more about compound libraries available from Tocris.

Technical Data for Roflumilast

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for Roflumilast

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

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.

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

Molarity Calculator

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Reconstitution Calculator

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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

If you know of a relevant reference for Roflumilast, please let us know.

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Citations for Roflumilast

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Currently there are no citations for Roflumilast. Do you know of a great paper that uses Roflumilast from Tocris? Please let us know.

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Literature in this Area

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