Roflumilast

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.

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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.

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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.
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]

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 <1 mg/mL
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol 30 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02363335 Completed Healthy Volunteers National Institute on Aging (NIA)|National Institutes of Health Clinical Center (CC) January 26, 2015 Phase 1
NCT01862029 Recruiting Obesity National Heart, Lung, and Blood Institute (NHLBI)|National Institutes of Health Clinical Center (CC) April 25, 2013 Phase 1|Phase 2
NCT02835716 Recruiting Alzheimer Disease Millennium Magnetic Technologies, LLC September 2016 --
NCT02671942 Recruiting Chronic Obstructive Pulmonary Disease Jiangsu Chia-tai Tianqing Pharmaceutical Co.,Ltd March 2016 Phase 2
NCT02451540 Recruiting Pulmonary Disease, Chronic Obstructive FLUIDDA nv September 2015 Phase 2
NCT02340520 Completed COPD UConn Health December 2014 Phase 3

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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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PDE Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID