Home Metabolism PDE inhibitor Roflumilast For research use only.

Roflumilast

Synonyms: APTA 2217, B9302-107, BY 217, BYK 20869

Roflumilast is a selective inhibitor of PDE4 with IC50 of 0.2-4.3 nM in a cell-free assay.

Roflumilast Chemical Structure

Roflumilast Chemical Structure

CAS No. 162401-32-3

Purity & Quality Control

Roflumilast Related Products

Signaling Pathway

PDE Signaling Pathways

PDE Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
PBMC Function assay Inhibition of TNFalpha production in LPS-stimulated human PBMC preincubated before LPS challenge measured after 4 hrs by enzyme immunoassay, IC50=2e-05 μM 19256507
sf21 cells Function assay Inhibition of human full length PDE4A4 expressed in baculovirus infected sf21 cells, IC50=0.35 nM 23806553
HEK293 cells Function assay 15 min Inhibition of PDE4 expressed in HEK293 cells coexpressing cyclic nucleotide gated ion channel mutant assessed as inhibition of NECA-induced cAMP production treated 15 mins before NECA challenge measured after 45 mins by FLIPR assay 20378348
Click to View More Cell Line Experimental Data

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)		 Click to View More Targets
0.2 nM 0.7 nM 0.7 nM 0.9 nM 3 nM
In vitro
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]
In Vivo
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05684744 Completed
Psoriasis
Cairo University
 January 9 2023 Phase 2|Phase 3
NCT04655313 Completed
Psoriasis|Plaque Psoriasis
Arcutis Biotherapeutics Inc.
 November 30 2020 Phase 2
NCT04279119 Completed
Plaque Psoriasis
Arcutis Biotherapeutics Inc.
 March 10 2020 Phase 1
NCT04156191 Completed
Atopic Dermatitis (Eczema)
Arcutis Biotherapeutics Inc.
 December 23 2019 Phase 1
NCT03762330 Unknown status
Chronic Obstructive Pulmonary Disease
Fundacio d''Investigacio en Atencio Primaria Jordi Gol i Gurina|Institut Catala de Salut
 January 19 2019 Not Applicable

Chemical Information & Solubility

Molecular Weight 403.21 Formula

C17H14Cl2F2N2O3
CAS No. 162401-32-3 SDF Download Roflumilast SDF
Smiles C1CC1COC2=C(C=CC(=C2)C(=O)NC3=C(C=NC=C3Cl)Cl)OC(F)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 81 mg/mL ( (200.88 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 15 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

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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.

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