Discontinued Product

Roflumilast (Cat. No. 6641) has been withdrawn from sale for commercial reasons.
Description: Potent and selective PDE4 inhibitor
Chemical Name: 3-(Cyclopropylmethoxy)-N-(3,5-dichloro-4-pyridinyl)-4-(difluoromethoxy)benzamide
Purity: ≥98% (HPLC)
Citations (2)

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
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.

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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Keywords: Roflumilast, Roflumilast supplier, Roflumilast, potent, selective, phosphodiesterase, 4, PDE4, inhibitors, inhibits, PDE4A, PDE4B, PDE4C, PDE4D, Phosphodiesterases, 6641, Tocris Bioscience

2 Citations for Roflumilast

Citations are publications that use Tocris products. Selected citations for Roflumilast include:

Martin J et al (2020) Optical Mapping of cAMP Signaling at the Nanometer Scale. Cell 182 1519-1530.e17 PMID: 32846156

Ronald M et al (2022) FGF1 and insulin control lipolysis by convergent pathways. Cell Metab 34 171-183.e6 PMID: 34986332

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