Roflumilast N-oxide

Roflumilast N-oxide is a phosphodiesterase 4 inhibitor. Roflumilast N-oxide is the active metabolite of roflumilast. Roflumilast N-Oxide in Combination with Formoterol Enhances the Antiinflammatory Effect of Dexamethasone in Airway Smooth Muscle Cells. Roflumilast n-oxide associated with PGE2 prevents the neutrophil elastase-induced production of chemokines by epithelial cells. (In Vitro) :Roflumilast N-oxide at 2 nM partly mitigates the cigarette smoke extract (CSE) -induced epithelial to mesenchymal transition (EMT) in WD-HBEC in vitro. Roflumilast N-oxide (2 nM) reverses the compromised expression of E-cadherin transcripts following CSE by 45%. The expression of collagen type I is abrogated by Roflumilast N-oxide (2 nM) . The epithelial cell phenotype appears protected when cells are co-incubated with Roflumilast N-oxide (2 nM) . Pre-incubation with Roflumilast N-oxide (2 nM) also partly attenuates the nuclear translocation of β-catenin. (In Vivo) :Single treatment of db/db mice with 10 mg/kg Roflumilast N-oxide enhances plasma glucagon-like peptide-1 (GLP-1) 4-fold. Chronic treatment of db/db mice with Roflumilast N-oxide at 3 mg/kg shows prevention of disease progression. Roflumilast-N-oxide abolishes the increase in blood glucose, reduces the increment in HbA1c by 50% and doubles fasted serum insulin compare with vehicle, concomitants with preservation of pancreatic islet morphology. Furthermore, Roflumilast-N-oxide amplifies forskolin-induced insulin release in primary islets. Roflumilast-N-oxide also shows stronger glucose-lowering effects than its parent compound.

292135-78-5

Roflumilast N-oxide

Pharmacology & Drug Discovery

>98% (HPLC)

DMSO : 320 mg/mL 763.34 mM

Clc3c[n+] ([O-]) cc (Cl) c3NC (=O) c2ccc (OC (F) F) c (OCC1CC1) c2

C17H14Cl2F2N2O4

419.21

Storage temperature: -20°C. Stability: ≥ 2 years

For research use only.