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Doxofylline
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。
Doxofylline图片
CAS NO:69975-86-6
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
100mg电议
200mg电议
500mg电议

产品名称
多索茶碱
产品介绍
Doxofylline 是一种口服有效的PDE IV抑制剂,也是A1AR拮抗剂。Doxofylline 通过抑制线粒体 ROS 的产生,以及改善多种细胞途径 (包括NLRP3-TXNIP炎症体的激活) 来减轻上皮细胞的炎症。Doxophylline 可用于哮喘、慢性阻塞性肺病和支气管痉挛的研究。
生物活性

Doxofylline is an orally activePDE IVinhibitor andA1ARantagonist. Doxofylline reduces inflammation in epithelial cells via inhibiting mitochondrial ROS production and amelioration of multiple cellular pathways (NLRP3-TXNIPinflammasome activation). Doxophylline can be used in studies of asthma, chronic obstructive pulmonary disease, and bronchospasm[1][2][3].

IC50& Target

Adenosine A1 receptor, phosphodiesterase IV[1][2][3].

体外研究
(In Vitro)

Doxofylline (5, 10 μM; 48 h) shows potent protection against LPS-induced epithelial inflammation by reducing PGE2, NO release, and decreasing mitochondrial ROS generation in 16HBE cells[1].
Doxofylline (5, 10 μM; 48 h) suppresses LPS-induced expression of NADPH oxidase subunits and TXNIP 16HBE cells[1].
Doxofylline (5, 10 μM; 48 h) inhibits LPS-induced NLRP3 inflammasome activation and secretion of IL-1b and IL-18, as well as mitigates LPS-mediated SIRT1 reduction[1].
Doxofylline (0.1-10 μM; 15 min) significantly reduces fMLP-induced leukocyte migration in BM cells (fMLP: Formyl-Methionyl-Leucyl-Phenylalanine)[2].

Cell Viability Assay[1]

Cell Line:16HBE cells
Concentration:5, 10 μM
Incubation Time:48 h
Result:Weakened LPS-induced NO and PGE2in a dose-dependent manner.
Exerted dose-dependent inhibition on LPS-induced mitochondrial ROS production and NADPH oxidase subunits expression.
Suppressed LPS-induced TXNIP expression and NLRP3 inflammasome activation at the protein level in a dose-dependent manner.
Inhibited LPS-induced secretion of IL-1b and IL-18.

Cell Viability Assay[2]

Cell Line:BM cells (from naive mice)
Concentration:0.1-10 μM
Incubation Time:15 min (pretreat)
Result:Notably surpressed positive migration of BM cells in response to fMLP.
体内研究
(In Vivo)

Doxofylline (0.3, 1 mg/kg; i.p.; single) inhibits LPS-induced inflammation in the lungs of mice[2].
Doxofylline (0.3 mg/kg; i.p.; pre-treat; single) notably reduces the adhesion of cells to the vascular tissue and surpresses the expression of LPS-induced ICAM-1 in vivo[2].

Animal Model:Male BALB/c mice (6 to 8-week-old)[2].
Dosage:0.3, 1 mg/kg
Administration:Intraperitoneal injection; single.
Result:Significantly inhibited the migration of neutrophils and the release of IL-6 and TNF-a into the lung lumen.
Increased the bone marrow leukocyte numbers to levels similar to those seen in the saline-treated group.
Notably reduced the number of circulating leukocytes in comparison to LPS-treated mice.
Significantly reduced accumulation of neutrophils in the peribronchial area.
Animal Model:Male BALB/c mice (6 to 8-week-old)[2].
Dosage:0.3 mg/kg
Administration:Intraperitoneal injection; pre-treat; single.
Result:Significantly reduced the adhesion of cells to the vascular tissue, but not the rolling of cells along the vessel wall in mice.
Significantly reduced the expression of ICAM-1 induced by LPS.
Clinical Trial
分子量

266.25

性状

Solid

Formula

C11H14N4O4

CAS 号

69975-86-6

中文名称

多索茶碱

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 50 mg/mL(187.79 mM;Need ultrasonic)

H2O : 25 mg/mL(93.90 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM3.7559 mL18.7793 mL37.5587 mL
5 mM0.7512 mL3.7559 mL7.5117 mL
10 mM0.3756 mL1.8779 mL3.7559 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: PBS

    Solubility: 65 mg/mL (244.13 mM); Clear solution; Need ultrasonic and warming and heat to 60℃

  • 2.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 2.5 mg/mL (9.39 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.39 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: ≥ 2.5 mg/mL (9.39 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.39 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 4.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.5 mg/mL (9.39 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.39 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。