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| 100mg |
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Purity: ≥98%
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.
| ln Vitro |
In vitro, cigarette smoke extract (CSE)-induced epithelial-mesenchymal transition (EMT) in WD-HBEC was partially inhibited by roflumilast N-oxide at a concentration of 2 nM. After CSE, 45% of the reduced E-cadherin transcript expression is restored by roflumilast N-oxide (2 nM). The expression of type I collagen is eliminated by roflumilast N-oxide (2 nM). There seems to be protection for the epithelial cell phenotype when roflumilast N-oxide (2 nM) was added to the cells. Additionally, β-catenin nuclear translocation is partially attenuated by preincubation with roflumilast N-oxide (2 nM) [2].
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| ln Vivo |
Plasma glucagon-like peptide-1 (GLP-1) increased four-fold in db/db mice treated once with 10 mg/kg roflumilast N-oxide. Roflumilast N-oxide at a dose of 3 mg/kg was found to stop the disease from progressing in db/db mice when given over an extended period of time. When roflumilast-N-oxide was used as a carrier, it preserved islet shape and lowered blood glucose and HbA1c increases by 50% and 50%, respectively. It also doubled fasting serum insulin. Moreover, in primary islets, roflumilast-N-oxide improved forskolin-induced insulin release. Additionally, compared to its parent molecule, rolumilast-N-oxide has stronger hypoglycemia effects [3].
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| References |
[1]. Victoni T, et al. 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,et al. 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, et al. The glucose-lowering effects of the PDE4 inhibitors roflumilast and roflumilast-N-oxide in db/db mice. Diabetologia. 2012 Oct;55(10):2779-2788 |
| Molecular Formula |
C17H14CL2F2N2O4
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|---|---|
| Molecular Weight |
419.2069
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| CAS # |
292135-78-5
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| Related CAS # |
Roflumilast;162401-32-3;Roflumilast Impurity E;1391052-76-8
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| SMILES |
ClC1=C([H])N(C([H])=C(/C/1=N\C(C1C([H])=C([H])C(=C(C=1[H])OC([H])([H])C1([H])C([H])([H])C1([H])[H])OC([H])(F)F)=O)Cl)O[H]
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~596.36 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.96 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.96 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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