1. Metabolic Enzyme/Protease
  2. Phosphodiesterase (PDE)
  3. Roflumilast N-oxide

Roflumilast N-oxide 

Cat. No.: HY-100639 Purity: 99.69%
Handling Instructions

Roflumilast N-oxide is a PDE type 4 inhibitor.

For research use only. We do not sell to patients.

Roflumilast N-oxide Chemical Structure

Roflumilast N-oxide Chemical Structure

CAS No. : 292135-78-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 266 In-stock
Estimated Time of Arrival: December 31
2 mg USD 144 In-stock
Estimated Time of Arrival: December 31
5 mg USD 288 In-stock
Estimated Time of Arrival: December 31
10 mg USD 480 In-stock
Estimated Time of Arrival: December 31
25 mg USD 960 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1680 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Roflumilast N-oxide:

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Description

Roflumilast N-oxide is a PDE type 4 inhibitor.

IC50 & Target

PDE type 4[1]

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[2].

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[3].

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 320 mg/mL (763.34 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3854 mL 11.9272 mL 23.8544 mL
5 mM 0.4771 mL 2.3854 mL 4.7709 mL
10 mM 0.2385 mL 1.1927 mL 2.3854 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[3]

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[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

419.21

Formula

C₁₇H₁₄Cl₂F₂N₂O₄

CAS No.

292135-78-5

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Roflumilast N-oxide
Cat. No.:
HY-100639
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Roflumilast N-oxide

Cat. No.: HY-100639