292135-78-5
基本信息
羅氟司特雜質(zhì)I
羅氟司特氧化物
羅氟司特N氧化物
羅氟司特氮氧化物
羅氟斯特N-氧化物
羅氟司特-IM K
羅氟斯特N氧化物雜質(zhì)
3-環(huán)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
3,5-二氯-4-[3-(環(huán)丙基甲氧基)-4-(二氟甲氧基)苯甲酰胺]吡啶1-氧化物
Roflumilast-6
RofluMilast N-Oxide
3-(CyclopropylMethoxy)-N
3,5-dichloro-4-(3-(cyclopr
3,5-dichloro-4-(3-(cyclopropylMethoxy)-4-(difluoroMethoxy)benzaMido)pyridine 1-oxide
N-(3,5-Dichloro-1-oxopyridin-4-yl)-4-difluoroMethoxy-3-cyclopropyl- MethoxybenzaMide
3-(CyclopropylMethoxy)-N-(3,5-dichloro-1-oxido-4-pyridinyl)-4-(difluoroMethoxy)benzaMide
3-(CYCLOPROPYLMETHOXY)-N-(3,5-DICHLORO-1-OXO-1Λ-PYRIDIN-4-YL)-4-(DIFLUOROMETHOXY)BENZAMIDE
Benzamide,3-(cyclopropylmethoxy)-N-(3,5-dichloro-1-oxido-4-pyridinyl)-4-(difluoromethoxy)-
物理化學(xué)性質(zhì)
常見問題列表
PDE type 4
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.
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.