Roflumilast (B9302-107)

For research use only.

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

16 publications

Roflumilast (B9302-107) Chemical Structure

CAS No. 162401-32-3

Roflumilast (APTA 2217, B9302-107, BY 217, BYK 20869) is a selective inhibitor of PDE4 with IC50 of 0.2-4.3 nM in a cell-free assay.

Selleck's Roflumilast (B9302-107) has been cited by 16 publications

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 (B9302-107) purchased from Selleck.

Purity & Quality Control

Choose Selective PDE Inhibitors

Biological Activity

Description Roflumilast (APTA 2217, B9302-107, BY 217, BYK 20869) 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 NFTVcVRHfW6ldHnvckBie3OjeR?= MkLETY5pcWKrdHnvckBw\iCWTl\hcJBp[SCycn;keYN1cW:wIHnuJGxRWy2|dHnteYxifGWmIHj1cYFvKFCETVOgdJJmcW6ldXLheIVlKGKnZn;y[UBNWFNiY3jhcIxmdmenIH3lZZN2emWmIHHmeIVzKDRiaILzJIJ6KGWweont[UBqdW23bn;hd5NigSxiSVO1NF0z\S1yNTFOwG0> MV6xPVI2PjVyNx?=
sf21 cells M3TXb2Z2dmO2aX;uJIF{e2G7 NHPv[HhKdmirYnn0bY9vKG:oIHj1cYFvKG[3bHygcIVv\3SqIGDESVRCPCCneIDy[ZN{\WRiaX6gZoFkfWyxdnnyeZMhcW6oZXP0[YQhe2Z{MTDj[YxteyxiSVO1NF0xNjN3IH7N NUHz[Gx1OjN6ME[1OVM>
HEK293 cells NVrqbVJETnWwY4Tpc44h[XO|YYm= NIDHS5gyPSCvaX6= MlzETY5pcWKrdHnvckBw\iCSRFW0JIV5eHKnc4Pl[EBqdiCKRVuyPVMh[2WubIOgZ49mgHC{ZYPzbY5oKGO7Y3zpZ{BvfWOuZX;0bYRmKGejdHXkJIlwdiClaHHucoVtKG23dHHueEBie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJG5GS0FvaX7keYNm\CClQV3QJJBzd2S3Y4Tpc44hfHKnYYTl[EAyPSCvaX7zJIJm\m:{ZTDOSWNCKGOqYXzs[Y5o\SCvZXHzeZJm\CCjZoTldkA1PSCvaX7zJIJ6KE[OSWDSJIF{e2G7 NF3VT4kzODN5OEO0PC=>

... 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)
Water Insoluble
Ethanol '15 mg/mL
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, BY 217, BYK 20869
Smiles C1CC1COC2=C(C=CC(=C2)C(=O)NC3=C(C=NC=C3Cl)Cl)OC(F)F

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04279119 Completed Drug: ARQ-151- cream 0.3% Plaque Psoriasis Arcutis Biotherapeutics Inc. March 10 2020 Phase 1
NCT04156191 Recruiting Drug: ARQ-151 cream 0.15%|Drug: ARQ-151 cream 0.05% Atopic Dermatitis (Eczema) Arcutis Biotherapeutics Inc. December 23 2019 Phase 1
NCT03762330 Recruiting Behavioral: COPD structured self-management plan. Chronic Obstructive Pulmonary Disease Jordi Gol i Gurina Foundation|Institut Catala de Salut January 19 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

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

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

Related PDE Products

Tags: buy Roflumilast (B9302-107) | Roflumilast (B9302-107) supplier | purchase Roflumilast (B9302-107) | Roflumilast (B9302-107) cost | Roflumilast (B9302-107) manufacturer | order Roflumilast (B9302-107) | Roflumilast (B9302-107) distributor
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID