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Formula | C17H14Cl2F2N2O3 |
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Molecular Weight | 403.21 | CAS No. | 162401-32-3 | |
Solubility (25°C)* | In vitro | DMSO | 81 mg/mL (200.88 mM) | |
Ethanol | 21 mg/mL (52.08 mM) | |||
Water | Insoluble | |||
* <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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | Roflumilast is a selective inhibitor of PDE4 with IC50 of 0.2-4.3 nM in a cell-free assay. | |||||||||||
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Targets |
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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] |
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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] |
Data from [J Mass Spectrom, 2012, 47, 1612-1619 ]
Functional rescue of CFTR in rectal organoids from patients carrying R334W variant by CFTR modulators and PDE4 inhibitor Roflumilast [ Respir Investig, 2024, 62(3):455-461] | PubMed: 38547757 |
PDE4D binds and interacts with YAP to cooperatively promote HCC progression [ Cancer Lett, 2022, 541:215749] | PubMed: 35597479 |
Long-Acting β2 Adrenergic Receptor Agonist Ameliorates Imiquimod-Induced Psoriasis-Like Skin Lesion by Regulating Keratinocyte Proliferation and Apoptosis [ Front Pharmacol, 2022, 13:865715] | PubMed: 35795567 |
Phosphodiesterase 4A confers resistance to PGE2-mediated suppression in CD25+ /CD54+ NK cells [ EMBO Rep, 2021, e51329] | PubMed: 33480074 |
Roflumilast prevents ischemic stroke-induced neuronal damage by restricting GSK3β-mediated oxidative stress and IRE1α/TRAF2/JNK pathway [ Free Radic Biol Med, 2021, 163:281-296] | PubMed: 33359910 |
Actionable Cytopathogenic Host Responses of Human Alveolar Type 2 Cells to SARS-CoV-2 [ Mol Cell, 2020, 80(6):1104-1122.e9] | PubMed: 33259812 |
Hyperinsulinemia promotes heterologous desensitization of β2 adrenergic receptor in airway smooth muscle in obesity. [ FASEB J, 2020, 10.1096/fj.201800688RR] | PubMed: 31960515 |
Transforming Growth Factor-β1 Decreases β2-Agonist-induced Relaxation in Human Airway Smooth Muscle. [ Am J Respir Cell Mol Biol, 2019, 61(2):209-218] | PubMed: 30742476 |
Pharmacological and molecular dynamics analyses of differences in inhibitor binding to human and nematode PDE4: Implications for management of parasitic nematodes [ PLoS One, 2019, 14(3):e0214554] | PubMed: 30917179 |
Phenotypic, chemical and functional characterization of cyclic nucleotide phosphodiesterase 4 (PDE4) as a potential anthelmintic drug target. [ PLoS Negl Trop Dis, 2017, 11(7):e0005680] | PubMed: 28704396 |
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