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Roflumilast N-oxide

MCE 国际站：Roflumilast N-oxide

品牌：MedChemExpress (MCE)

货号：HY-100639

CAS 号：292135⁻⁷8-5

生物活性：罗氟司特 N-氧化物是一种 PDE 4 型抑制剂。

体外研究(In Vitro)：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]. MCE尚未独立确认这些方法的准确性。 仅供参考。

体内研究(In Vivo)：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]. MCE尚未独立确认这些方法的准确性。 仅供参考。

分子量：419.21

Formula：C17H14Cl2F2N2O4

性状：固体

颜色：White to off-white

中文名称：罗氟司特N-氧化物

运输条件：美国大陆地区的室温；其他地区可能有所不同。

储存方式：粉末 -20°C 3年

Cell Assay [1]：A549细胞经洗涤后，在添加了抗生素、L-谷氨酰胺和HEPES的无血清F-12K培养基中培养过夜。饥饿处理后的细胞用中性粒细胞弹性蛋白酶（NE）或溶剂（PBS）孵育30分钟，用PBS洗涤后，继续在无血清F-12K培养基中培养。刺激后，分别于24小时收集细胞上清液（用于细胞因子测定），并于2小时后收集细胞沉淀（用于mRNA表达分析）。或者，在加入NE之前，A549细胞先用罗氟司特N-氧化物（RNO）（浓度分别为0.1 µM、0.3 µM和1 µM）或溶剂（0.01% DMSO）预孵育2小时。所有实验均在无血清培养基中进行，每个处理设置三个复孔，并至少重复三次。孵育结束后，收集培养上清液并储存于-80°C，直至进行后续分析[1]。 MCE 尚未独立确认这些方法的准确性。仅供参考。

Animal Administration [3]：At 7 weeks of age, 16 h fasting mice receive a single oral dose of vehicle (4% methocel) or 10 mg/kg Roflumilast-N-oxide, and a glucose bolus of 2 g/kg body weight is co-administered as a physiological initiator for glucagon-like peptide-1 (GLP-1) secretion. Plasma GLP-1 is analyzed 60 min before, and 10 and 60 min after administration of Roflumilast-N-oxide and glucose. The effect of Roflumilast-N-oxide on plasma GLP-1 is also investigated in the absence of the glucose bolus[3]. MCE尚未独立确认这些方法的准确性。 仅供参考。

文献引用：MCE 顾客使用本产品发表 1 篇科研文献

提供质量检测报告：Data Sheet、SDS、COA、HNMR、LCMS、产品使用指南

产品活性：Roflumilast N-oxide 是一个 PDE 4 型抑制剂。

IC50 & Target：PDE type 4[1]

相关产品：IBMX | IBMX | IBMX (Standard) | Roflumilast N-oxide (Standard) | Phorbol 12-myristate 13-acetate | Phorbol 12-myristate 13-acetate (Standard) | Nerandomilast | Trametinib | Docetaxel | Docetaxel (Standard) | Fulvestrant | SR-18292

热门产品线：抑制剂 | 稳定性同位素标记物 | 脂质 | 糖类

Trending products：Inhibitors | Isotope-Labeled Compounds | Lipids | Saccharides

参考文献：
[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.