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Roflumilast

SKU: orb1310022
FeaturedFeatured Product

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

Pharmacology & Drug Discovery

Images & Validation

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Roflumilast

Key Properties

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CAS Number162401-32-3
MW403.21
Purity>98%
FormulaC17H14N2Cl2F2O3
SMILESO(CC1CC1)C2=C(OC(F)F)C=CC(C(NC=3C(Cl)=CN=CC3Cl)=O)=C2
TargetPDE (Phosphodiesterase)
SolubilitySoluble in DMSO (up to 25 mg/ml)

Bioactivity

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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.
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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).
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Storage & Handling

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Storage-20°C
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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BYK-20869

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Quality Guarantee

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at [email protected].

Compound Identifiers

PubChem CID
449193 ↗

Key Properties

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No computed properties available.

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Roflumilast (orb1310022)

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10 mg
¥ 2,210.00
50 mg
¥ 4,420.00
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