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Roflumilast N-oxide

Cat. No. M9882
Roflumilast N-oxide Structure
Size Price Availability Quantity
5mg USD 88  USD88 In stock
10mg USD 132  USD132 In stock
25mg USD 230  USD230 In stock
50mg USD 380  USD380 In stock
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Quality Control & Documentation
Biological Activity

Roflumilast N-oxide is a phosphodiesterase 4 inhibitor. 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.

Chemical Information
Molecular Weight 419.21
Formula C17H14Cl2F2N2O4
CAS Number 292135-78-5
Solubility (25°C) DMSO ≥ 100 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Tatiana Victoni, et al. Int Immunopharmacol. Roflumilast n-oxide associated with PGE2 prevents the neutrophil elastase-induced production of chemokines by epithelial cells

[2] Javier Milara, et al. COPD. 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

[3] S Vollert, et al. Diabetologia. The glucose-lowering effects of the PDE4 inhibitors roflumilast and roflumilast-N-oxide in db/db mice

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