Roflumilast

For research use only.

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

11 publications

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  
10mM (1mL in DMSO) USD 101 In stock
USD 90 In stock
USD 170 In stock
USD 370 In stock
USD 570 In stock
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Selleck's Roflumilast has been cited by 11 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 purchased from Selleck.

Purity & Quality Control

Choose Selective PDE Inhibitors

Biological Activity

Description Roflumilast is a selective inhibitor of PDE4 with IC50 of 0.2-4.3 nM in a cell-free assay.
Targets
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 M{PFemZ2dmO2aX;uJIF{e2G7 MmHMTY5pcWKrdHnvckBw\iCWTl\hcJBp[SCycn;keYN1cW:wIHnuJGxRWy2|dHnteYxifGWmIHj1cYFvKFCETVOgdJJmcW6ldXLheIVlKGKnZn;y[UBNWFNiY3jhcIxmdmenIH3lZZN2emWmIHHmeIVzKDRiaILzJIJ6KGWweont[UBqdW23bn;hd5NigSxiSVO1NF0z\S1yNTFOwG0> M1vTNlE6OjV4NUC3
sf21 cells Ml23SpVv[3Srb36gZZN{[Xl? MnTHTY5pcWKrdHnvckBw\iCqdX3hckBnfWyuIHzlcod1cCCSRFW0RVQh\XiycnXzd4VlKGmwIHLhZ5Vtd3[rcoXzJIlv\mWldHXkJJNnOjFiY3XscJMtKEmFNUC9NE4{PSCwTR?= M2OwcVI{QDB4NUWz
HEK293 cells NGHXT4VHfW6ldHnvckBie3OjeR?= M4n0bVE2KG2rbh?= MkLHTY5pcWKrdHnvckBw\iCSRFW0JIV5eHKnc4Pl[EBqdiCKRVuyPVMh[2WubIOgZ49mgHC{ZYPzbY5oKGO7Y3zpZ{BvfWOuZX;0bYRmKGejdHXkJIlwdiClaHHucoVtKG23dHHueEBie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJG5GS0FvaX7keYNm\CClQV3QJJBzd2S3Y4Tpc44hfHKnYYTl[EAyPSCvaX7zJIJm\m:{ZTDOSWNCKGOqYXzs[Y5o\SCvZXHzeZJm\CCjZoTldkA1PSCvaX7zJIJ6KE[OSWDSJIF{e2G7 MYiyNFM4QDN2OB?=

... 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]

Protocol

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
Formula

C17H14Cl2F2N2O3

CAS No. 162401-32-3
Storage powder
in solvent
Synonyms APTA 2217, B9302-107, BY 217, BYK 20869
Smiles FC(F)OC1=CC=C(C=C1OCC2CC2)C(=O)NC3=C(Cl)C=NC=C3Cl

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 (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)
% DMSO % % Tween 80 % ddH2O
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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)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / 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 )

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

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
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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 Recruiting Drug: ARQ-151- cream 0.3% Plaque Psoriasis Arcutis Biotherapeutics Inc. March 10 2020 Phase 1
NCT04156191 Recruiting Drug: ARQ-151 cream 0.15% Atopic Dermatitis (Eczema) Arcutis Biotherapeutics Inc. December 23 2019 Phase 1
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

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

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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