Roflumilast

SKU: orb1310022

Description

Roflumilast is a selective, long-acting PDE4 inhibitor that elevates intracellular cAMP levels, exhibiting anti-inflammatory and potential antineoplastic properties. It is widely used in research on COPD, psoriasis, and cancer, with applications in both in vitro cellular assays and in vivo animal models.

Research Area

Infectious Disease & Virology, Metabolism Research

Key Properties

• CAS Number: 162401-32-3
• MW: 403.21
• Purity: >99.99% (May vary between batches)
• Formula: C₁₇H₁₄Cl₂F₂N₂O₃
• SMILES: O(CC1CC1)C2=C(OC(F)F)C=CC(C(NC=3C(Cl)=CN=CC3Cl)=O)=C2
• Target: PDE,RSV
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:12 mg/mL (29.76 mM);DMSO:250 mg/mL (620.02 mM);10% DMSO+90% Corn Oil:2.5 mg/mL (6.2 mM)

Bioactivity

• Target IC50:
  PDE4B2:0.2 nM|PDE4A1:0.7 nM|PDE4C1:3 nM|PDE4B1:0.7 nM|PDE4A4:0.9 nM
• In Vivo:
  In vivo experiments demonstrated that Roflumilast reduces oxidative stress. It also confers a degree of resistance to pneumonia associated with COPD in animal models. In mouse lungs exposed to tobacco for seven months, Roflumilast (5 mg/kg/day) led to significant reductions in macrophages, neutrophils, B cells, dendritic cells, CD8+ T cells, and CD4+ T cells by 82%, 78%, 100%, 48%, 88%, and 98%, respectively. Following a 14-day intratracheal administration of bleomycin, Roflumilast (5 mg/kg/day) moderately decreased the augmentation of hydroperoxides in the mice's bronchoalveolar lavage fluid. Post-bleomycin treatment, dosages of Roflumilast proportionately reduced total pulmonary hydroxyproline content, with 5 mg/kg/day inhibiting by 47%, and additionally diminished pulmonary fibrotic damage and transcription of αI(I) collagen.
• In Vitro:
  In vitro experiments demonstrate that Roflumilast exhibits immunomodulatory and anti-inflammatory activities. It inhibits the activation of CD4+ T cells by anti-CD28 and anti-CD3 antibodies (IC30: 7 nM), and suppresses the synthesis of IL-2 (IC20: 1 nM), IL-4 (IC30: 7 nM), IL-5 (IC25: 13 nM), and IFN-γ (IC35: 8 nM). Additionally, Roflumilast inhibits LTB4 synthesis in human neutrophils (IC50: 2 nM) and blocks ROS generation stimulated by fMLP in eosinophils and neutrophils, with an IC35 of 7 nM and 4 nM, respectively. It also impedes the production of TNF-α in monocytes (IC40: 21 nM) induced by lipopolysaccharide, as well as in monocyte-derived dendritic cells (IC20: 5 nM).

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BY217, BY-217, BYK 20869, BYK20869, BYK-20869, BY 217, APTA 2217, APTA2217, APTA-2217, B9302-107, Inhibitor, inhibit, Roflumilast, RSV, Respiratory syncytial virus, Phosphodiesterase (PDE), phosphodiesterase, PDE4C1, PDE4B2, PDE4B1, PDE4A1, PDE4A4

Compound Identifiers

PubChem CID

449193