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Roflumilast

Catalog No. T1024 CAS 162401-32-3

Synonyms: B9302-107, BYK 20869, APTA 2217, BY 217

Roflumilast (APTA 2217) is an orally available, long-acting inhibitor of phosphodiesterase (PDE) type 4 (PDE4), with anti-inflammatory and potential antineoplastic activities. Upon administration, roflumilast and its active metabolite roflumilast N-oxide selectively and competitively bind to and inhibit PDE4, which leads to an increase of both intracellular levels of cyclic-3', 5'-adenosine monophosphate (cAMP) and cAMP-mediated signaling.

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Roflumilast, CAS 162401-32-3

Pack Size	Availability	Price/USD
5 mg	In stock	$ 50.00
10 mg	In stock	$ 67.00
25 mg	In stock	$ 119.00
50 mg	In stock	$ 189.00
100 mg	In stock	$ 264.00
1 mL * 10 mM (in DMSO)	In stock	$ 54.00

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Purity: 100.00%

Purity: 99.64%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Roflumilast (APTA 2217) is an orally available, long-acting inhibitor of phosphodiesterase (PDE) type 4 (PDE4), with anti-inflammatory and potential antineoplastic activities. Upon administration, roflumilast and its active metabolite roflumilast N-oxide selectively and competitively bind to and inhibit PDE4, which leads to an increase of both intracellular levels of cyclic-3', 5'-adenosine monophosphate (cAMP) and cAMP-mediated signaling.
Targets&IC50	PDE4B1:0.7 nM, PDE4A4:0.9 nM, PDE4C1:3 nM, PDE4A1:0.7 nM, PDE4B2:0.2 nM
In vitro	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 vivo	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).
Kinase Assay	PDE activity is determined with some modifications. The assay mixture contain 50 mM Tris (pH 7.4), 5 mM MgCl2, 0.5 μM cAMP or cGMP, and [3H]cAMP or [3H]cGMP (about 30,000 cpm/assay), the indicated concentration of the inhibitor and an aliquot of the enzyme solution at a final assay volume of 200 μL. Stock solutions of the compounds are diluted 1:100 (v/v) in the Tris buffer mentioned above; appropriate dilutions are prepared in 1% (v/v) DMSO/Tris buffer, which are diluted 1:2 (v/v) in the assays to obtain the desired final concentrations of the inhibitors at a DMSO concentration of 0.5% (v/v). DMSO itself affected none of the PDE activities. After preincubation for 5 min at 37°C, the reaction is started by the addition of substrate (cAMP or cGMP) and the assays are incubated for further 15 min at 37°C. Then 50 μL of 0.2 N HCl is added to stop the reaction and the assays are left on ice for about 10 min. Following incubation with 25 μg of 5′-nucleotidase (Crotalus atrox snake venom) for 10 min at 37°C, the assays are loaded on QAE Sephadex A-25 (1 mL of bed volume in Poly-Prep chromatography columns). The columns are eluted with 2 mL of 30 mM ammonium formate (pH 6.0) and the eluate is counted for radioactivity. Results are corrected for blank values (measured in the presence of denatured protein) that are below 5% of total radioactivity. The amount of cyclic nucleotides hydrolyzed did not exceed 30% of the original substrate concentration[3].

Synonyms	B9302-107, BYK 20869, APTA 2217, BY 217
Molecular Weight	403.21
Formula	C17H14Cl2F2N2O3
CAS No.	162401-32-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 12 mg/mL (29.8 mM)

DMSO: 75 mg/mL (186 mM)

References and Literature

1. Hatzelmann A, et al. Pulm Pharmacol Ther, 2010, 23(4), 235-256. 2. Hatzelmann A, et al. J Pharmacol Exp Ther, 2001, 297(1), 267-279. 3. Martorana PA, et al. BMC Pulm Med, 2008, 8:17. 4. Cortijo J, et al. Br J Pharmacol, 2009, 156(3), 534-544. 6. Ding H, et al. Treatment of obesity-associated overactive bladder by the phosphodiesterase type-4 inhibitor roflumilast. Int Urol Nephrol. 2017 Jul 29.

Citations

1. Chen L, Ye T, Wang X, et al.Decoction on Major Depressive Disorder based on Network Pharmacology and Molecular Docking.Combinatorial Chemistry & High Throughput Screening.2023, 26(9): 1701-1728.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Neurodegenerative Disease Compound Library Anti-Cancer Approved Drug Library EMA Approved Drug Library Anti-Cancer Drug Library Drug Repurposing Compound Library Inhibitor Library Anti-Cancer Clinical Compound Library Anti-Cancer Active Compound Library Bioactive Compounds Library Max Pediatric Drug Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Roflumilast 162401-32-3 Metabolism Microbiology/Virology PDE RSV BY217 Respiratory syncytial virus BYK20869 B9302-107 BYK 20869 Phosphodiesterase (PDE) APTA 2217 BY-217 BY 217 inhibit APTA2217 Inhibitor APTA-2217 BYK-20869 inhibitor

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