Catalog No.S2131 Synonyms: APTA 2217, B9302-107, BY 217, BYK 20869
Molecular Weight(MW): 403.21
Roflumilast is a selective inhibitor of PDE4 with IC50 of 0.2-4.3 nM in a cell-free assay.
Cited by 7 Publications
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|Description||Roflumilast is a selective inhibitor of PDE4 with IC50 of 0.2-4.3 nM in a cell-free assay.|
Roflumilast displays anti-inflammatory and immunomodulatory in vitro. Roflumilast inhibits LTB4 synthesis in human neutrophil with IC50 of 2 nM. Roflumilast inhibits fMLP-stimulated ROS formation as luminol-enhanced CL in human neutrophils or eosinophils with IC35 of 4 nM, and 7 nM, repectively. Roflumilast inhibits LPS-stimulated TNF-α synthesis in monocytes with IC40 of 21 nM. Roflumilast inhibits TNF-α synthesis in monocyte-derived dendritic cells with IC20 of 5 nM. Rolfumilast inhibits anti-CD3 and anti-CD28 antibody-stimulated proliferation of CD4+ T cells with IC30 of 7 nM. Rolfumilast inhibits anti-CD3 and anti-CD28 antibody-stimulated synthesis of IL-2, IL-4, IL-5, and IFN-v in CD4+ T cells with IC20 of 1 nM, IC30 of 7 nM, IC25 of 13 nM, and IC35 of 8 nM, respectively. 
|In vivo||Roflumilast is activity against pulmonary inflammatory response related to COPD in animal model. Roflumilast (5 mg/kg/day) induces reduction of neutrophils, macrophages, DC, B-cells, CD4+ T cells, CD8+ T cells in the lung of mice exposed to tobacco smoke for 7 month by 78%, 82%, 48%, 100%, 98%, and 88%, respectively.  Roflumilast is an efficient inhibitor of lung fibrotic remodeling. Roflumilast dose-dependently diminishes total lung hydroxyproline after bleomycin, attaining about 47% inhibition at 5 mg/kg/day, paralleled by a reduction in lung αI(I) collagen transcripts and fibrotic lesions. Roflumilast reduces oxidative stress in vivo. Roflumilast (5 mg/kg/day) moderately reduces an increase in BAL fluid lipid hydroperoxides measured at day 14 after intratracheal bleomycin administration in mice. |
|In vitro||DMSO||81 mg/mL (200.88 mM)|
|Ethanol||15 mg/mL (37.2 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% propylene glycol
For best results, use promptly after mixing.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
|Synonyms||APTA 2217, B9302-107, BY 217, BYK 20869|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03762330||Not yet recruiting||Behavioral: COPD structured self-management plan.||Chronic Obstructive Pulmonary Disease||Jordi Gol i Gurina Foundation|Institut Catala de Salut||February 2019||Not Applicable|
|NCT01862029||Completed||Drug: Roflumilast||Obesity||National Heart Lung and Blood Institute (NHLBI)|National Institutes of Health Clinical Center (CC)||May 22 2013||Phase 1|Phase 2|
|NCT01354782||Completed||Drug: Roflumilast||Chronic Obstructive Pulmonary Disease||AstraZeneca||May 2011||Phase 1|
|NCT02187926||Completed||--||Chronic Obstructive Pulmonary Disease||AstraZeneca||May 2011||--|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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Frequently Asked Questions
Could you tell me which diluent you advise to use with S2131 for in vivo applications in mice?
For s2131, the in vivo formulation is 30% PEG400+0.5% Tween80+5% Propylene glycol up to 30mg/mL.