Roflumilast

Roflumilast (APTA-2217) is a selective PDE4 inhibitor with IC50s of 0.7, 0.9, 0.7, and 0.2 nM for PDE4A1, PDE4A4, PDE4B1, and PDE4B2, respectively, without affecting PDE1, PDE2, PDE3 or PDE5 isoenzymes from various cells.

Product Specifications

CAS Number

[162401-32-3]

Product Name Alternative

APTA-2217; BYK 20869; B9302-107

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Phosphodiesterase (PDE) ; RSV

Type

Reference compound

Related Pathways

Anti-infection; Metabolic Enzyme/Protease

Applications

COVID-19-anti-virus

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/Roflumilast.html

Purity

99.98

Solubility

DMSO : ≥ 50 mg/mL|H2O : < 0.1 mg/mL (ultrasonic)

Smiles

O=C(NC1=C(Cl)C=NC=C1Cl)C2=CC=C(OC(F)F)C(OCC3CC3)=C2

Molecular Formula

C17H14Cl2F2N2O3

Molecular Weight

403.21

Precautions

H302, H315, H319, H335

References & Citations

[2]Rabe KF. Update on roflumilast, a phosphodiesterase 4 inhibitor for the treatment of chronic obstructive pulmonary disease. Br J Pharmacol. 2011 May;163 (1) :53-67.|[3]Hatzelmann A, et al. Anti-inflammatory and immunomodulatory potential of the novel PDE4 inhibitor roflumilast in vitro. J Pharmacol Exp Ther. 2001 Apr;297 (1) :267-79.|[4]Richmond BW, et al. Airway bacteria drive a progressive COPD-like phenotype in mice with polymeric immunoglobulin receptor deficiency. Nat Commun. 2016 Apr 5;7:11240.|[5]Ding H, et al. Treatment of obesity-associated overactive bladder by the phosphodiesterase type-4 inhibitor roflumilast. Int Urol Nephrol. 2017 Jul 29.|[1]Hatzelmann A, et al. The preclinical pharmacology of roflumilast--a selective, oral phosphodiesterase 4 inhibitor in development for chronic obstructive pulmonary disease. Pulm Pharmacol Ther. 2010 Aug;23 (4) :235-56.