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Roflumilast N-oxide

Catalog No. T4462   CAS 292135-78-5

Roflumilast N-oxide is an inhibitor of PDE type 4.

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Roflumilast N-oxide Chemical Structure
Roflumilast N-oxide, CAS 292135-78-5
Pack Size Availability Price/USD Quantity
1 mg In stock $ 30.00
2 mg In stock $ 44.00
5 mg In stock $ 68.00
10 mg In stock $ 101.00
25 mg In stock $ 173.00
50 mg In stock $ 288.00
100 mg In stock $ 369.00
500 mg In stock $ 885.00
1 mL * 10 mM (in DMSO) In stock $ 63.00
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Purity: 99.65%
Purity: 99.55%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Roflumilast N-oxide is an inhibitor of PDE type 4.
Targets&IC50 PDE type 4:
In vitro Roflumilast N-oxide partly mitigates the cigarette smoke extract (CSE)-induced epithelial to mesenchymal transition (EMT) at 2 nM in WD-HBEC in vitro. Roflumilast N-oxide (2 nM) reverses the compromised expression of E-cadherin transcripts following CSE by 45%. Roflumilast N-oxide (2 nM) abrogates the expression of collagen type I. 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. Moreover, Roflumilast-N-oxide amplifies forskolin-induced insulin release in primary islets. Besides, Roflumilast-N-oxide shows stronger glucose-lowering effects than its parent compound.
Cell Research A549 cells are washed and cultured overnight in serum-free F-12 K medium supplemented with antibiotics, L-glutamine and HEPES. The starved cells are incubated with Neutrophil elastase (NE) for 30 min or vehicle (PBS), washed with PBS and then cultured in serum free F-12 K. After stimulation, cell supernatants are collected at 24 h (for cytokine measurements) and cell pellets are collected after 2 h (for mRNA expression analysis). Alternatively, A549 cells are pre-incubated for 2 h with Roflumilast N-oxide (RNO) (at 0.1 μM, 0.3 μM and 1 μM), vehicle (DMSO 0.01%) prior to the addition of NE. All experiments are performed in serum-free medium in triplicate and are repeated at least three times. At the end of the incubation period, culture supernatants are harvested and stored at -80°C until further analysis
Animal Research At 7 weeks of age, 16 h fasting mice receive a single oral dose of vehicle (4% methocel) or 10 mg/kg Roflumilast-N-oxide, and a glucose bolus of 2 g/kg body weight is co-administered as a physiological initiator for glucagon-like peptide-1 (GLP-1) secretion. Plasma GLP-1 is analyzed 60 min before, and 10 and 60 min after administration of Roflumilast-N-oxide and glucose. The effect of Roflumilast-N-oxide on plasma GLP-1 is also investigated in the absence of the glucose bolus
Molecular Weight 419.21
Formula C17H14Cl2F2N2O4
CAS No. 292135-78-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 320 mg/mL

TargetMolReferences and Literature

1. Victoni T,etal.Roflumilast n-oxide associated with PGE2 prevents the neutrophil elastase-induced production of chemokines by epithelial cells.Int Immunopharmacol. 2016 Jan;30:1-8. 2. Milara J,etal.Simvastatin Increases the Ability of Roflumilast N-oxide to Inhibit Cigarette Smoke-Induced Epithelial to Mesenchymal Transition in Well-differentiated Human Bronchial Epithelial Cells in vitro.COPD. 2015 Jun;12(3):320-31. 3. Vollert S,etal.The glucose-lowering effects of the PDE4 inhibitors roflumilast and roflumilast-N-oxide in db/db mice.Diabetologia. 2012 Oct;55(10):2779-2788.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Neurodegenerative Disease Compound Library FDA-Approved & Pharmacopeia Drug Library Bioactive Lipid Compound Library Bioactive Compounds Library Max FDA-Approved Drug Library Metabolism Compound Library NO PAINS Compound Library Anti-Cardiovascular Disease Compound Library Human Metabolite Library Immunology/Inflammation Compound Library

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Keywords

Roflumilast N-oxide 292135-78-5 Metabolism PDE Phosphodiesterase (PDE) Roflumilast N oxide Roflumilast Noxide Inhibitor inhibit inhibitor

 

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