3-(CYCLOPROPYLMETHOXY)-N-(3,5-DICHLORO-1-OXO-1Λ-PYRIDIN-4-YL)-4-(DIFLUOROMETHOXY)BENZAMIDE
Roflumilast N-Oxide
CAS: 292135-78-5
Molecular Formula: C17H14Cl2F2N2O4
3-(CYCLOPROPYLMETHOXY)-N-(3,5-DICHLORO-1-OXO-1Λ-PYRIDIN-4-YL)-4-(DIFLUOROMETHOXY)BENZAMIDE - Names and Identifiers
3-(CYCLOPROPYLMETHOXY)-N-(3,5-DICHLORO-1-OXO-1Λ-PYRIDIN-4-YL)-4-(DIFLUOROMETHOXY)BENZAMIDE - Physico-chemical Properties
| Molecular Formula | C17H14Cl2F2N2O4 |
| Molar Mass | 419.21 |
| Density | 1.56±0.1 g/cm3(Predicted) |
| Melting Point | 181 °C |
| Boling Point | 519.7±50.0 °C(Predicted) |
| Solubility | Chloroform, Ethyl Acetate |
| Appearance | Solid |
| Color | Off White to Light Peach |
| pKa | 9.19±0.70(Predicted) |
| Storage Condition | Sealed in dry,Store in freezer, under -20°C |
| In vitro study | 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. |
| In vivo study | 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 HbA 1c 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-(CYCLOPROPYLMETHOXY)-N-(3,5-DICHLORO-1-OXO-1Λ-PYRIDIN-4-YL)-4-(DIFLUOROMETHOXY)BENZAMIDE - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.385 ml | 11.927 ml | 23.854 ml |
| 5 mM | 0.477 ml | 2.385 ml | 4.771 ml |
| 10 mM | 0.239 ml | 1.193 ml | 2.385 ml |
| 5 mM | 0.048 ml | 0.239 ml | 0.477 ml |
Last Update：2024-01-02 23:10:35
3-(CYCLOPROPYLMETHOXY)-N-(3,5-DICHLORO-1-OXO-1Λ-PYRIDIN-4-YL)-4-(DIFLUOROMETHOXY)BENZAMIDE - Reference Information
| biological activity | Roflumilast N-oxide is a PDE type 4 inhibitor. |
| Target | PDE type 4 |
Last Update：2024-04-10 22:29:15
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Product Name: Roflumilast Impurity 6 Visit Supplier Webpage Request for quotationCAS: 292135-78-5
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Spot supply
Product Name: Roflumilast N-Oxide Visit Supplier Webpage Request for quotationCAS: 292135-78-5
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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