中文名 | 罗氟司特氮氧化物 |
英文名 | Roflumilast N-Oxide |
别名 | 罗氟司特杂质I 罗氟司特氧化物 罗氟司特N氧化物 罗氟司特氮氧化物 罗氟司特-IM K 罗氟斯特N-氧化物 3-环丙甲氧基-4-二氟甲氧基-N-(3,5-二氯-4-基苯基-1-氧化物)苯甲酰胺 3-(环丙甲氧基)-N-(3,5-二氯-1-氧代吡啶-4-基)-4-(二氟甲氧基)苯甲酰胺 |
英文别名 | RofluMilast N-Oxide Roflumilast N-Oxide 3,5-dichloro-4-(3-(cyclopr N-(3,5-Dichloro-1-oxopyridin-4-yl)-4-difluoroMethoxy-3-cyclopropyl-MethoxybenzaMide 3,5-dichloro-4-(3-(cyclopropylMethoxy)-4-(difluoroMethoxy)benzaMido)pyridine 1-oxide 3-(CyclopropylMethoxy)-N-(3,5-dichloro-1-oxido-4-pyridinyl)-4-(difluoroMethoxy)benzaMide Benzamide,3-(cyclopropylmethoxy)-N-(3,5-dichloro-1-oxido-4-pyridinyl)-4-(difluoromethoxy)- 3-(CYCLOPROPYLMETHOXY)-N-(3,5-DICHLORO-1-OXO-1Λ-PYRIDIN-4-YL)-4-(DIFLUOROMETHOXY)BENZAMIDE 3-(cyclopropylmethoxy)-N-(3,5-dichloro-1-hydroxypyridin-4-ylidene)-4-(difluoromethoxy)benzamide |
CAS | 292135-78-5 |
EINECS | 604-604-1 |
化学式 | C17H14Cl2F2N2O4 |
分子量 | 419.21 |
密度 | 1.56±0.1 g/cm3(Predicted) |
熔点 | 181 °C |
沸点 | 519.7±50.0 °C(Predicted) |
溶解度 | 氯仿,乙酸乙酯 |
酸度系数 | 9.19±0.70(Predicted) |
存储条件 | Sealed in dry,Store in freezer, under -20°C |
外观 | 固体 |
颜色 | Off White to Light Peach |
体外研究 | 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. |
体内研究 | 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. |
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 |
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