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 6 Publications
Purity & Quality Control
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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)|
|Water||slightly soluble or insoluble|
|In vivo||Add solvents individually and in order:
30% PEG400+0.5% Tween80+5% propylene glycol
* 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||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02363335||Completed||Healthy Volunteers||National Institute on Aging (NIA)|National Institutes of Health Clinical Center (CC)||January 26, 2015||Phase 1|
|NCT01862029||Recruiting||Obesity||National Heart, Lung, and Blood Institute (NHLBI)|National Institutes of Health Clinical Center (CC)||April 25, 2013||Phase 1|Phase 2|
|NCT02835716||Recruiting||Alzheimer Disease||Millennium Magnetic Technologies, LLC||September 2016||--|
|NCT02671942||Recruiting||Chronic Obstructive Pulmonary Disease||Jiangsu Chia-tai Tianqing Pharmaceutical Co.,Ltd||March 2016||Phase 2|
|NCT02451540||Recruiting||Pulmonary Disease, Chronic Obstructive||FLUIDDA nv||September 2015||Phase 2|
|NCT02340520||Completed||COPD||UConn Health||December 2014||Phase 3|
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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