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Roflumilast N-oxide

产品编号 T4462 CAS 292135-78-5

Roflumilast N-oxide 是一种 PDE 4 型抑制剂。

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Roflumilast N-oxide, CAS 292135-78-5

规格	价格/CNY	货期
1 mg	￥ 655	现货
2 mg	￥ 957	现货
5 mg	￥ 1,660	现货
10 mg	￥ 2,890	现货
25 mg	￥ 4,860	现货
50 mg	￥ 6,920	现货
100 mg	￥ 9,360	现货
500 mg	￥ 18,700	现货
1 mL * 10 mM (in DMSO)	￥ 1,530	现货

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Roflumilast N-oxide is an inhibitor of PDE type 4.
靶点活性	PDE Ⅳ:
体外活性	Roflumilast N-oxide partly mitigates the cigarette smoke extract (CSE)-induced epithelial to mesenchymal transition (EMT) at 2 nM in WD-HBEC in vitro. Roflumilast N-oxide (2 nM) reverses the compromised expression of E-cadherin transcripts following CSE by 45%. Roflumilast N-oxide (2 nM) abrogates the expression of collagen type I. 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.
体内活性	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. Moreover, Roflumilast-N-oxide amplifies forskolin-induced insulin release in primary islets. Besides, Roflumilast-N-oxide shows stronger glucose-lowering effects than its parent compound.
细胞实验	A549 cells are washed and cultured overnight in serum-free F-12 K medium supplemented with antibiotics, L-glutamine and HEPES. The starved cells are incubated with Neutrophil elastase (NE) for 30 min or vehicle (PBS), washed with PBS and then cultured in serum free F-12 K. After stimulation, cell supernatants are collected at 24 h (for cytokine measurements) and cell pellets are collected after 2 h (for mRNA expression analysis). Alternatively, A549 cells are pre-incubated for 2 h with Roflumilast N-oxide (RNO) (at 0.1 μM, 0.3 μM and 1 μM), vehicle (DMSO 0.01%) prior to the addition of NE. All experiments are performed in serum-free medium in triplicate and are repeated at least three times. At the end of the incubation period, culture supernatants are harvested and stored at -80°C until further analysis
动物实验	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

分子量	419.21
分子式	C17H14Cl2F2N2O4
CAS No.	292135-78-5

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 50 mg/mL (119.27 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3854 mL	11.9272 mL	23.8544 mL	59.636 mL
	5 mM	0.4771 mL	2.3854 mL	4.7709 mL	11.9272 mL
	10 mM	0.2385 mL	1.1927 mL	2.3854 mL	5.9636 mL
	20 mM	0.1193 mL	0.5964 mL	1.1927 mL	2.9818 mL
	50 mM	0.0477 mL	0.2385 mL	0.4771 mL	1.1927 mL
	100 mM	0.0239 mL	0.1193 mL	0.2385 mL	0.5964 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Victoni T,etal.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,etal.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,etal.The glucose-lowering effects of the PDE4 inhibitors roflumilast and roflumilast-N-oxide in db/db mice.Diabetologia. 2012 Oct;55(10):2779-2788.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Roflumilast N-oxide 292135-78-5 Metabolism PDE Phosphodiesterase (PDE) Roflumilast N oxide Roflumilast Noxide Inhibitor inhibit inhibitor

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Roflumilast N-oxide

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords