Roflumilast (B9302-107)

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

For research use only.

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.

Roflumilast (B9302-107) Chemical Structure

CAS No. 162401-32-3

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

Purity & Quality Control

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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.
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

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 NWXHbXl1TnWwY4Tpc44h[XO|YYm= M3rqTGlvcGmkaYTpc44hd2ZiVF7GZYxxcGFicILv[JVkfGmxbjDpckBNWFNvc4TpcZVt[XSnZDDoeY1idiCSQl3DJJBz\WmwY4XiZZRm\CCkZX\vdoUhVFCVIHPoZYxt\W6pZTDt[YF{fXKnZDDh[pRmeiB2IHjyd{BjgSCnbor5cYUhcW2vdX7vZZN{[XluIFnDOVA:OmVvMEWg{txO MmDxNVkzPTZ3MEe=
sf21 cells M{XGcGZ2dmO2aX;uJIF{e2G7 MlfYTY5pcWKrdHnvckBw\iCqdX3hckBnfWyuIHzlcod1cCCSRFW0RVQh\XiycnXzd4VlKGmwIHLhZ5Vtd3[rcoXzJIlv\mWldHXkJJNnOjFiY3XscJMtKEmFNUC9NE4{PSCwTR?= MnPPNlM5ODZ3NUO=
HEK293 cells MnjiSpVv[3Srb36gZZN{[Xl? NGLFZoIyPSCvaX6= NEm1T4VKdmirYnn0bY9vKG:oIGDESVQh\XiycnXzd4VlKGmwIFjFT|I6OyClZXzsd{Bkd2W6cILld5NqdmdiY4njcIlkKG63Y3zlc5Rq\GViZ3H0[YQhcW:wIHPoZY5v\WxibYX0ZY51KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhVkWFQT3pcoR2[2WmIHPBUXAheHKxZIXjeIlwdiC2cnXheIVlKDF3IH3pcpMh[mWob4LlJG5GS0FiY3jhcIxmdmenIH3lZZN2emWmIHHmeIVzKDR3IH3pcpMh[nliRlzJVHIh[XO|YYm= M4XhcVIxOzd6M{S4
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 (from reference)

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
Formula

C17H14Cl2F2N2O3

CAS No. 162401-32-3
Storage 3 years -20°C powder
2 years -80°C in solvent
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)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

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.

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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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