RofluMilast N-Oxide NEW
| Price | $8 | $3 | $2 |
| Package | 1kg | 100kg | 1000kg |
| Min. Order: | 1kg |
| Supply Ability: | g-kg-tons, free sample is available |
| Update Time: | 2024-04-25 |
Product Details
| Product Name: RofluMilast N-Oxide | CAS No.: 292135-78-5 |
| Min. Order: 1kg | Purity: 99% |
| Supply Ability: g-kg-tons, free sample is available | Release date: 2024/04/25 |
| Lead time: In stock | Packaging: bottle/drum/bucket/IBC, as request. |
| Delivery: By sea, by air, by express | Origin: Manufacturer |
| Contact person: Jessica |
1. Product information
| Name | 3-(cyclopropylmethoxy)-N-(3,5-dichloro-1-hydroxypyridin-4-ylidene)-4-(difluoromethoxy)benzamide |
|---|---|
| Synonym | More Synonyms |
| Description | Roflumilast N-oxide is a PDE type 4 inhibitor. |
|---|---|
| Related Catalog | Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphodiesterase (PDE) Research Areas >> Inflammation/Immunology |
| Target | PDE type 4[1] |
| In Vitro | Roflumilast N-oxide at 2 nM partly mitigates the cigarette smoke extract (CSE)-induced epithelial to mesenchymal transition (EMT) in WD-HBEC in vitro. Roflumilast N-oxide (2 nM) reverses the compromised expression of E-cadherin transcripts following CSE by 45%. The expression of collagen type I is abrogated by Roflumilast N-oxide (2 nM). The epithelial cell phenotype appears protected when cells are co-incubated with Roflumilast N-oxide (2 nM). Pre-incubation with Roflumilast N-oxide (2 nM) also partly attenuates the nuclear translocation of β-catenin[2]. |
| In Vivo | Single treatment of db/db mice with 10 mg/kg Roflumilast N-oxide enhances plasma glucagon-like peptide-1 (GLP-1) 4-fold. Chronic treatment of db/db mice with Roflumilast N-oxide at 3 mg/kg shows prevention of disease progression. Roflumilast-N-oxide abolishes the increase in blood glucose, reduces the increment in HbA1c by 50% and doubles fasted serum insulin compare with vehicle, concomitants with preservation of pancreatic islet morphology. Furthermore, Roflumilast-N-oxide amplifies forskolin-induced insulin release in primary islets. Roflumilast-N-oxide also shows stronger glucose-lowering effects than its parent compound[3]. |
| Cell Assay | A549 cells are washed and cultured overnight in serum-free F-12 K medium supplemented with antibiotics, L-glutamine and HEPES. The starved cells are incubated with Neutrophil elastase (NE) for 30 min or vehicle (PBS), washed with PBS and then cultured in serum free F-12 K. After stimulation, cell supernatants are collected at 24 h (for cytokine measurements) and cell pellets are collected after 2 h (for mRNA expression analysis). Alternatively, A549 cells are pre-incubated for 2 h with Roflumilast N-oxide (RNO) (at 0.1 μM, 0.3 μM and 1 μM), vehicle (DMSO 0.01%) prior to the addition of NE. All experiments are performed in serum-free medium in triplicate and are repeated at least three times. At the end of the incubation period, culture supernatants are harvested and stored at -80°C until further analysis[1]. |
| Animal Admin | At 7 weeks of age, 16 h fasting mice receive a single oral dose of vehicle (4% methocel) or 10 mg/kg Roflumilast-N-oxide, and a glucose bolus of 2 g/kg body weight is co-administered as a physiological initiator for glucagon-like peptide-1 (GLP-1) secretion. Plasma GLP-1 is analyzed 60 min before, and 10 and 60 min after administration of Roflumilast-N-oxide and glucose. The effect of Roflumilast-N-oxide on plasma GLP-1 is also investigated in the absence of the glucose bolus[3]. |
| References | [1]. Victoni T, et al. Roflumilast n-oxide associated with PGE2 prevents the neutrophil elastase-induced production of chemokines by epithelial cells. Int Immunopharmacol. 2016 Jan;30:1-8. [2]. Milara J,et al. Simvastatin Increases the Ability of Roflumilast N-oxide to Inhibit Cigarette Smoke-Induced Epithelial to Mesenchymal Transition in Well-differentiated Human Bronchial Epithelial Cells in vitro. COPD. 2015 Jun;12(3):320-31. [3]. Vollert S, et al. The glucose-lowering effects of the PDE4 inhibitors roflumilast and roflumilast-N-oxide in db/db mice. Diabetologia. 2012 Oct;55(10):2779-2788. |
| Density | 1.6±0.1 g/cm3 |
|---|---|
| Boiling Point | 519.7±50.0 °C at 760 mmHg |
| Melting Point | 181 °C |
| Molecular Formula | C17H14Cl2F2N2O4 |
| Molecular Weight | 419.207 |
| Flash Point | 268.1±30.1 °C |
| Exact Mass | 418.029877 |
| PSA | 73.05000 |
| LogP | 1.43 |
| Vapour Pressure | 0.0±1.4 mmHg at 25°C |
| Index of Refraction | 1.616 |
2. Packaging
For powders: normal is 25kgs/Drum or bag, or larger/smaller package as request.
For liquids: normal 25kgs/drum, 180-300kgs/bucket, or IBC, determined by the nature of the product.
Or smaller package 1kg/bottle, 10kgs/bottle as request.
3. Shipping
4. Contact information
For more details, pls contact us freely.
Mob: 86 17630978909
WhatsApp/Skype/Wechat/LINE: 86 17630978909
Company Profile Introduction
Henan Fengda Chemical Co., Ltd. is located in the High-tech Development Zone of Henan Province. Specializing in the production and sales of various fine chemical products required for industrial production, including chemical raw materials, organic raw materials, petrochemicals, chemical reagents, solvents, catalysts, and additives, etc.
You may like
Recommended supplier
| Product name | Price | Suppliers | Update time | |
|---|---|---|---|---|
| $0.00/5mg |
VIP3Y
|
TargetMol Chemicals Inc.
|
2024-10-23 | |
| $0.00/1g |
VIP1Y
|
BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.
|
2024-09-29 | |
| $10.00/1KG |
VIP4Y
|
Hebei Chuanghai Biotechnology Co,.LTD
|
2024-08-21 | |
| $30.00/1mg |
VIP5Y
|
TargetMol Chemicals Inc.
|
2024-10-30 |
China
- Since: 2023-02-10
- Address: Room 01, 2288 E05, Building 14, East Henan University, Science and Technology Park, 279 Xisanhuan Ro
INQUIRY