罗氟司特N-氧化物
中文名称 | 罗氟司特N-氧化物 |
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中文同义词 | 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;罗氟司特氮氧化物;罗氟司特N氧化物;罗氟司特氧化物;罗氟司特-IM K;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;罗氟司特杂质I;罗氟斯特N氧化物杂质 |
英文名称 | RofluMilast N-Oxide |
英文同义词 | RofluMilast N-Oxide;3-(CyclopropylMethoxy)-N-(3,5-dichloro-1-oxido-4-pyridinyl)-4-(difluoroMethoxy)benzaMide;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;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;3,5-dichloro-4-(3-(cyclopr;3-(cyclopropylmethoxy)-N-(3,5-dichloro-1-hydroxypyridin-4-ylidene)-4-(difluoromethoxy)benzamide |
CAS号 | 292135-78-5 |
分子式 | C17H14Cl2F2N2O4 |
分子量 | 419.21 |
EINECS号 | 604-604-1 |
相关类别 | 罗氟司特;标准品;对照品-杂质对照品;杂质对照品;Heterocycles;Inhibitors;Intermediates & Fine Chemicals;Metabolites & Impurities;Pharmaceuticals |
Mol文件 | 292135-78-5.mol |
结构式 | ![]() |
罗氟司特N-氧化物 性质
熔点 | 181 °C |
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沸点 | 519.7±50.0 °C(Predicted) |
密度 | 1.56±0.1 g/cm3(Predicted) |
储存条件 | Sealed in dry,Store in freezer, under -20°C |
溶解度 | 可溶于氯仿、乙酸乙酯 |
形态 | 固体 |
酸度系数(pKa) | 9.19±0.70(Predicted) |
颜色 | 灰白色至浅桃色 |
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.
安全信息
海关编码 | 2933.39.4100 |
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更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/08/19 | HY-100639 | Roflumilast N-oxide | 1 mg | 800元 | |
2024/08/19 | HY-100639 | RofluMilast N-Oxide Roflumilast N-oxide | 292135-78-5 | 10mM * 1mLin DMSO | 1845元 |