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.
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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||30% PEG400+0.5% Tween80+5% propylene glycol||30 mg/mL|
* 1 mg/ml means slightly soluble or insoluble.
* 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|
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