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CAS No.: 292135-78-5

Roflumilast N-oxide/罗氟司特氮氧化物 Catalog No. CSN23672

Synonyms: 罗氟司特N-氧化物

Roflumilast N-oxide, an active metabolite of roflumilast, is an inhibitor of phosphodiesterase 4 (PDE4). It can be combined with formoterol to enhance the antiinflammatory effect of dexamethasone.

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生物活性

描述Roflumilast N-oxide is a PDE type 4 inhibitor. Co-administration of rifampicin and roflumilast led to a reduction in total PDE4 inhibitory activity of roflumilast by about 58%^[2]. The PDE4 inhibitor roflumilast N-oxide acts (over) additively with simvastatin to prevent CSE-induced EMT (epithelial-mesenchymal transition) in WD-HBEC (well-differentiated human bronchial epithelial cells) in vitro^[3]. Roflumilast-N-oxide fosters the expression of SPs (Surfactant proteins) in human AEC-II (alveolar epithelial cells type II) via increase of intracellular cAMP levels potentially contributing to improved alveolar host defence and enhanced resolution of inflammation^[4]. Roflumilast N-oxide concentration-dependently triggered a rapid and persistent increase in ciliary beat frequency (CBF) and reversed the decrease in CBF following cigarette smoke extract (CSE). Roflumilast N-oxide protected differentiated human bronchial epithelial cells from reduced CBF and loss of ciliated cells following CSE^[5]. 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. 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^[6].
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.3854 mL
- 11.9272 mL
- 23.8544 mL
- 5 mM
- 0.4771 mL
- 2.3854 mL
- 4.7709 mL
- 10 mM
- 0.2385 mL
- 1.1927 mL
- 2.3854 mL

技术信息

CAS号

292135-78-5

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H14Cl2F2N2O4

运输

蓝冰

分子量

419.21

别名

罗氟司特N-氧化物

溶解度

DMSO	430.0 mg/mL (1025.7 mM)
Water	insoluble

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Roflumilast N-oxide/罗氟司特氮氧化物 Catalog No. CSN23672

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