Catalog No.S2131 Synonyms: APTA 2217, B9302-107, BY 217, BYK 20869

Roflumilast  Chemical Structure

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.

Size Price Stock Quantity  
In DMSO USD 101 In stock
USD 90 In stock
USD 170 In stock
USD 370 In stock
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1 Customer Review

  • Mean plasma concentration versus time after single dose oral administration of IC87114 and RFM in wistar rats( n = 6).

    J Mass Spectrom 2012 47, 1612-1619 . Roflumilast purchased from Selleck.

Purity & Quality Control

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Biological Activity

Description Roflumilast is a selective inhibitor of PDE4 with IC50 of 0.2-4.3 nM in a cell-free assay.
PDE4B2 [1]
(Cell-free assay)
PDE4A1 [1]
(Cell-free assay)
PDE4B1 [1]
(Cell-free assay)
PDE4A4 [1]
(Cell-free assay)
PDE4C1 [1]
(Cell-free assay)
0.2 nM 0.7 nM 0.7 nM 0.9 nM 3 nM
In vitro

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. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
PBMC MWrGeY5kfGmxbjDhd5NigQ>? NHvwRlJKdmirYnn0bY9vKG:oIGTOSoFteGijIIDyc4R2[3Srb36gbY4hVFCVLYP0bY12dGG2ZXSgbJVu[W5iUFLNR{BxemWrbnP1ZoF1\WRiYnXmc5JmKEySUzDjbIFtdGWwZ3WgcYVie3W{ZXSgZYZ1\XJiNDDodpMh[nliZX76fY1mKGmvbYXuc4F{e2G7LDDJR|UxRTKnLUC1JO69VQ>? MnTJNVkzPTZ3MEe=
sf21 cells NXK0RnpiTnWwY4Tpc44h[XO|YYm= NWrPXHRJUW6qaXLpeIlwdiCxZjDoeY1idiCodXzsJIxmdme2aDDQSGU1STRiZYjwdoV{e2WmIHnuJIJi[3Wub4\pdpV{KGmwZnXjeIVlKHOoMkGgZ4VtdHNuIFnDOVA:OC5|NTDuUS=> MXGyN|gxPjV3Mx?=
HEK293 cells MmjGSpVv[3Srb36gZZN{[Xl? M3j0OVE2KG2rbh?= M{LlSmlvcGmkaYTpc44hd2ZiUFTFOEBmgHC{ZYPz[YQhcW5iSFXLNlk{KGOnbHzzJINw\XiycnXzd4lv\yCleXPsbYMhdnWlbHXveIll\SCpYYTl[EBqd25iY3jhco5mdCCvdYThcpQh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBPTUODLXnu[JVk\WRiY1HNVEBxem:mdXP0bY9vKHS{ZXH0[YQhOTVibXnud{Bj\W[xcnWgUmVESSClaHHscIVv\2VibXXhd5Vz\WRiYX\0[ZIhPDVibXnud{BjgSCITFnQVkBie3OjeR?= M{jXeFIxOzd6M{S4

... Click to View More Cell Line Experimental Data

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. [3] 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. [4]


Solubility (25°C)

In vitro DMSO 81 mg/mL (200.88 mM)
Ethanol 15 mg/mL (37.2 mM)
Water Insoluble
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.
30 mg/mL

* 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.

Chemical Information

Molecular Weight 403.21


CAS No. 162401-32-3
Storage powder
in solvent
Synonyms APTA 2217, B9302-107, BY 217, BYK 20869

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Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01443845 Completed COPD|COPD Exacerbation|Lung Diseases|Respiratory Disorders|Pulmonary Disease|Chronic Obstructive Lung Diseases|Chronic Obstructive Airway Disease AstraZeneca September 30 2011 Phase 4
NCT03532490 Recruiting Asthma|Obesity Johns Hopkins University|American Lung Association|National Heart Lung and Blood Institute (NHLBI) August 3 2018 Phase 2
NCT03381573 Recruiting COPD AstraZeneca March 23 2017 --
NCT01862029 Completed Obesity National Heart Lung and Blood Institute (NHLBI)|National Institutes of Health Clinical Center (CC) May 22 2013 Phase 1|Phase 2
NCT03458546 Recruiting Lymphoma B-Cell Adolfo Enrique Diaz Duque|The University of Texas Health Science Center at San Antonio May 21 2018 Phase 1
NCT02835716 Recruiting Alzheimer Disease Millennium Magnetic Technologies LLC September 2016 --

Tech Support

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

  • Question 1:

    Could you tell me which diluent you advise to use with S2131 for in vivo applications in mice?

  • Answer:

    For s2131, the in vivo formulation is 30% PEG400+0.5% Tween80+5% Propylene glycol up to 30mg/mL.

PDE Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID