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RofluMilast N-Oxide

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RofluMilast N-Oxide

查看77 家供应商

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CAS No. 292135-78-5

分子式 C17H14Cl2F2N2O4

分子量 419.21

英文名称 RofluMilast N-Oxide

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

基本信息

产品名称

RofluMilast N-Oxide

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 No.

292135-78-5

分子式

C17H14Cl2F2N2O4

分子量

419.21

EINECS号

604-604-1

MDL NO.

MFCD04112984

MOL

292135-78-5.mol

性质

密度

1.56±0.1 g/cm3(Predicted)

形态

Solid

沸点

519.7±50.0 °C(Predicted)

熔点

181 °C

颜色

Off White to Light Peach

溶解度

Chloroform, Ethyl Acetate

酸度系数(pKa)

9.19±0.70(Predicted)

储存条件

Sealed in dry,Store in freezer, under -20°C

用途

靶点

PDE type 4

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.

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.

生物活性

Roflumilast N-oxide 是一个 PDE 4 型抑制剂。

安全信息