| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| Other Sizes |
|
Purity: ≥98%
Roflumilast (BY-217; APTA-2217; B 9302-107; BYK20869; Daxas; Daliresp) is a novel, highly potent, selective, and long-acting inhibitor of phosphodiesterase 4/PDE4 with potential anti-inflammatory activity. It inhibits PDE4 with IC50s of 0.2-4.3 nM in a cell-free assay. It has anti-inflammatory effects and is under development as an orally administered drug for the treatment of inflammatory conditions of the lungs such as asthma, and chronic obstructive pulmonary disease (COPD). In vitro studies show that roflumilast inhibits the production of inflammatory mediators in a variety of human immune cells, suggesting a role for reducing COPD-related inflammation.
| ln Vitro |
Roflumilast is a subnanomolar inhibitor of the majority of PDE4 splice variants tested and has no effect on PDE enzymes other than PDE4. With the exception of PDE4C (4C1, IC50=3 nM; 4C2, IC50= 4.3 nM), which is inhibited with somewhat lesser potency, it does not demonstrate PDE4 isoform selectivity [2]. A strong and specific PDE4 inhibitor is roflumast. At concentrations up to 10,000-fold, roflumilast does not affect other PDE isoenzymes, such as PDE1, PDE2, PDE3, or PDE5. This makes it a monoselective inhibitor of PDE4. Roflumilast inhibits the activity of human neutrophils. Roflumilast prevents monocyte-derived dendritic cells from synthesizing TNFα. Cytokine synthesis and CD4+ T cell proliferation are inhibited by rolfumilast. Up to 60% of proliferation can be inhibited by rolumilast at a potency (IC30) of 7 nM [3].
|
||
|---|---|---|---|
| ln Vivo |
Studies on animals using roflumilast have demonstrated that it decreases the build-up of neutrophils in bronchoalveolar lavage fluid following short-term tobacco smoke exposure in mice, rats, or guinea pigs; additionally, it eliminates the infiltration of inflammatory cells in the lung parenchyma of rats exposed to tobacco smoke for seven months [2]. In pIgR, rolumilast prevents the advancement of COPD?*? rats. 9-month-old WT or pIgR for these investigations?*? For three months, mice received oral gavage treatment with either 100 μg of Roflumilast (5 μg/g) or a vehicle (4% methylcellulose, 1.3% PEG400). Around the age of 12 months, the lungs were taken. When Roflumilast was administered to mice, minor airway wall remodeling did not advance as it did in vehicle-treated pIgR-/- animals. Surprisingly, pIgR aged 12 months who received rolumilast?*? Compared to 9-month-old pIgR, mice's emphysema index was lower.*? Roflumilast not only stops pulmonary emphysema from developing in this scenario, as demonstrated by the mice. appears to aid in the resolution of the emphysematous loss of lung parenchyma throughout the course of emphysema [4].
|
||
| Animal Protocol |
|
||
| References |
[1]. Hatzelmann A, et al. The preclinical pharmacology of roflumilast--a selective, oral phosphodiesterase 4 inhibitor in development for chronic obstructive pulmonary disease. Pulm Pharmacol Ther. 2010 Aug;23(4):235-56.
[2]. Rabe KF. Update on roflumilast, a phosphodiesterase 4 inhibitor for the treatment of chronic obstructive pulmonary disease. Br J Pharmacol. 2011 May;163(1):53-67. [3]. Hatzelmann A, et al. Anti-inflammatory and immunomodulatory potential of the novel PDE4 inhibitor roflumilast in vitro. J Pharmacol Exp Ther. 2001 Apr;297(1):267-79. [4]. Richmond BW, et al. Airway bacteria drive a progressive COPD-like phenotype in mice with polymeric immunoglobulin receptor deficiency. Nat Commun. 2016 Apr 5;7:11240. [5]. Ding H, et al. Treatment of obesity-associated overactive bladder by the phosphodiesterase type-4 inhibitor roflumilast. Int Urol Nephrol. 2017 Jul 29 |
| Molecular Formula |
C17H14CL2F2N2O3
|
|---|---|
| Molecular Weight |
403.2075
|
| CAS # |
162401-32-3
|
| Related CAS # |
Roflumilast N-oxide;292135-78-5;Roflumilast-d4 N-Oxide;1794760-31-8;Roflumilast Impurity E;1391052-76-8;Roflumilast-d4;1398065-69-4;Roflumilast-d3;1189992-00-4
|
| SMILES |
ClC1C([H])=NC([H])=C(C=1N([H])C(C1C([H])=C([H])C(=C(C=1[H])OC([H])([H])C1([H])C([H])([H])C1([H])[H])OC([H])(F)F)=O)Cl
|
| Synonyms |
Daliresp; BY217; BY-217; B 9302-107;BYK 20869;B-9302-107;APTA 2217, B9302-107, BY 217, BYK-20869; BYK20869; Daxas;
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.20 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 2: 30% PEG400+0.5% Tween80+5% propylene glycol:30 mg/mL (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4801 mL | 12.4005 mL | 24.8010 mL | |
| 5 mM | 0.4960 mL | 2.4801 mL | 4.9602 mL | |
| 10 mM | 0.2480 mL | 1.2400 mL | 2.4801 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05684744 | Completed | Drug: Roflumilast Drug: Methotrexate |
Psoriasis | Cairo University | January 9, 2023 | Phase 2 Phase 3 |
| NCT04322929 | Recruiting | Drug: Roflumilast Oral Tablet | Non-cystic Fibrosis Bronchiectasis | The University of Hong Kong | November 12, 2020 | Phase 2 |
| NCT04549870 | Completed | Drug: Roflumilast | Psoriasis | Bispebjerg Hospital | January 1, 2021 | Phase 2 |
| NCT04108377 | Terminated | Drug: Roflumilast Drug: Placebo |
Asthma | University of California, Davis | January 21, 2019 | Phase 1 |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA
