Roflumilast

Catalog No.S2131 Batch:S213101

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Technical Data

Formula

C17H14Cl2F2N2O3

Molecular Weight 403.21 CAS No. 162401-32-3
Solubility (25°C)* In vitro DMSO 81 mg/mL (200.88 mM)
Ethanol 15 mg/mL (37.2 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.)

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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)
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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 (from reference)

Customer Product Validation

Data from [J Mass Spectrom, 2012, 47, 1612-1619 ]

Selleck's Roflumilast has been cited by 20 publications

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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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.