Roflumilast

SKU: orb1310022

Description

Roflumilast

Research Area

Infectious Disease & Virology, Metabolism Research

Key Properties

• CAS Number: 162401-32-3
• MW: 403.21
• Purity: 99.86%
• 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