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Home > Products > Metabolism > PDE Inhibitor > Roflumilast 162401-32-3

Roflumilast 162401-32-3

Product Description

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Molecular Weight:

403.21 Roflumilast is a selective inhibitor of PDE4 with IC50 of 0.2-4.3 nM.






Biological Activity


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.


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. 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.

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