Doxofylline|69975-86-6|(多索茶碱)-陌孚医药/Medlife

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Doxofylline (Synonyms: 多索茶碱)

目录号: PC16497 纯度: ≥98%

CAS No. :69975-86-6

商品编号	规格	价格	会员价	是否有货	数量
PC16497-50mg	50mg	¥509.00	请登录
PC16497-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥637.00	请登录

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中文名称

Doxofylline

中文别名

多沙茶碱;1,3-二甲基-7-(1,3-二氧环戊基-2-基)甲基-3,7-二氢-1H-嘌呤-2,6-二酮;多索茶碱;2-(7'-茶碱甲基)-1,3-二氧戊环;DOXOFYLLINE 多索茶碱;多沙茶碱（多索茶碱）;多索茶碱 USP标准品;多索茶碱标准品;7-(1,3-二氧环戊-2-基甲基)茶碱;7-(1,3-二氧戊环-2-基甲基)-1,3-二甲黄嘌呤;7-(1,3-二氧戊环-2-基甲基)-1,3-二甲基-1H-嘌呤-2,6-二酮;7-(1,3-二氧戊环-2-基甲基)-1,3-二甲基黄嘌呤;7-(1,3-二氧戊环-2-基甲基)茶碱

英文名称

Doxofylline

英文别名

Doxofylline;7-(1,3-dioxolan-2-ylmethyl)-1,3-dimethylpurine-2,6-dione;Doxophylline;7-(1,3-dioxolan-2-ylmethyl)-theophyllin 3,7-dihydro-7-(1,3-dioxolan-2-ylmethyl)-1,3-dimethyl-1h-purine-6-dione;2-(7'-theophyllinemethyl)-1,3-dioxolane;7-(1,3-dioxolan-2-yl-methyl)3,7-dihydro-1,3-dimethyl-1H-purine-2,6-dione;7-(1,3-dioxolan-2-ylmethyl)theophylline;ABC 12;Ansimar;Dioxyfilline;Doxofilina [INN-Spanish];Doxofyllinum [INN-Latin];Maxivent;Ventax;7-(1,3-dioxolan-2-ylmethyl)-theophyllin;7-(1,3-Dioxolan-2-ylmethyl)-1,3-dimethyl-1H-purine-2,6-dione;7-(1,3-Dioxolan-2-ylmethyl)-1,3-dimethylxanthine;7-(1,3-Dioxolan-2-ylmethyl)-3,7-dihydro-1,3-dimethyl-1H-Purine-2,6-dione;Doxofylline [USAN:INN];ABC 12/3;MPM23GMO7Z;Theophylline, 7-(1,3-dioxolan-2-ylmethyl)-;HWXIGFIVGWUZAO-UHFFFAOYSA-N;2-(7'-Teofillinmetil)-1,3-diossolano [Italian];DSSTo

Cas No.

69975-86-6

分子式

C₁₁H₁₄N₄O₄

分子量

266.25

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

Doxofylline is an orally active PDE IV inhibitor and A1AR antagonist. Doxofylline reduces inflammation in epithelial cells via inhibiting mitochondrial ROS production and amelioration of multiple cellular pathways (NLRP3-TXNIP inflammasome activation). Doxophylline can be used in studies of asthma, chronic obstructive pulmonary disease, and bronchospasm.

性状

Solid

IC50 & Target[1][2]

Adenosine A1 receptor, phosphodiesterase IV.

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.
Doxofylline (5, 10 μM; 48 h) suppresses LPS-induced expression of NADPH oxidase subunits and TXNIP 16HBE cells.
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.
Doxofylline (0.1-10 μM; 15 min) significantly reduces fMLP-induced leukocyte migration in BM cells (fMLP: Formyl-Methionyl-Leucyl-Phenylalanine).

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

Cell Line:	16HBE cells
Concentration:	5, 10 μM
Incubation Time:	48 h
Result:	Weakened LPS-induced NO and PGE2 in 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

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.
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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male BALB/c mice (6 to 8-week-old).
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).
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.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

ClinicalTrial

参考文献

[1]. Jiao P, et al. The protective effect of doxofylline against lipopolysaccharides (LPS)-induced activation of NLRP3 inflammasome is mediated by SIRT1 in human pulmonary bronchial epithelial cells. Artif Cells Nanomed Biotechnol. 2020 Dec;48(1):687-694. [Information]

[2]. Riffo-Vasquez Y, et al. Doxofylline, a novofylline inhibits lung inflammation induced by lipopolysacharide in the mouse. Pulm Pharmacol Ther. 2014 Apr;27(2):170-8. [Information]

[3]. Shukla D, et al. Doxofylline: a promising methylxanthine derivative for the treatment of asthma and chronic obstructive pulmonary disease. Expert Opin Pharmacother. 2009 Oct;10(14):2343-56. [Information]

溶解度数据

体外研究:

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

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

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.7559 mL	18.7793 mL	37.5587 mL
5 mM	0.7512 mL	3.7559 mL	7.5117 mL
10 mM	0.3756 mL	1.8779 mL	3.7559 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

建议依照次序添加每种溶剂： PBS
Solubility: 65 mg/mL (244.13 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
2.

建议依照次序添加每种溶剂： 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 ddH?O 中，得到澄清透明的生理盐水溶液
3.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in 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 μL 20% 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.

建议依照次序添加每种溶剂： 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。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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