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Roflumilast N-oxide
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Roflumilast N-oxide图片
CAS NO:292135-78-5
规格:98%
分子量:419.21
包装与价格:
包装价格(元)
100mg电议
200mg电议
2mg电议
5mg电议
10mg电议
25mg电议
50mg电议

产品介绍
Roflumilast N-oxide 是一个 PDE 4 型抑制剂。
CAS:292135-78-5
分子式:C17H14Cl2F2N2O4
分子量:419.21
纯度:98%
存储:Store at -20°C

Background:

Roflumilast N-oxide is a PDE type 4 inhibitor. PDE type 4[1]


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[2].


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 HbA1c 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[3].


[1]. Victoni T, et al. Roflumilast n-oxide associated with PGE2 prevents the neutrophil elastase-induced production of chemokines by epithelial cells. Int Immunopharmacol. 2016 Jan;30:1-8. [2]. Milara J,et al. Simvastatin Increases the Ability of Roflumilast N-oxide to Inhibit Cigarette Smoke-Induced Epithelial to Mesenchymal Transition in Well-differentiated Human Bronchial Epithelial Cells in vitro. COPD. 2015 Jun;12(3):320-31. [3]. Vollert S, et al. The glucose-lowering effects of the PDE4 inhibitors roflumilast and roflumilast-N-oxide in db/db mice. Diabetologia. 2012 Oct;55(10):2779-2788.