Theophylline sodium acetate (Synonyms: 1,3-Dimethylxanthine sodium acetate; Theo-24 sodium acetate)

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Theophylline sodium acetate  (Synonyms: 1,3-Dimethylxanthine sodium acetate; Theo-24 sodium acetate)

Theophylline (1,3-Dimethylxanthine) sodium acetate 是有效的磷酸二酯酶 (PDE) 抑制剂，腺苷受体拮抗剂，和组蛋白脱乙酰酶 (HDAC) 活化剂。Theophylline (1,3-Dimethylxanthine) sodium acetate 抑制 PDE3 活性，放松气道平滑肌。Theophylline (1,3-Dimethylxanthine) sodium acetate 通过增加 IL-10 和抑制 NF-κ B进入细胞核而具有抗炎活性。Theophylline (1,3-Dimethylxanthine) sodium acetate 诱发细胞凋亡 (apoptosis)。Theophylline (1,3-Dimethylxanthine) sodium acetate 可用于哮喘和慢性阻塞性肺疾病 (COPD) 的研究。

Theophylline sodium acetate (Synonyms: 1,3-Dimethylxanthine sodium acetate; Theo-24 sodium acetate)

Theophylline sodium acetate Chemical Structure

CAS No. : 8002-89-9

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生物活性

Theophylline (1,3-Dimethylxanthine) sodium acetate is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline (1,3-Dimethylxanthine) sodium acetate inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) sodium acetate has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) sodium acetate induces apoptosis. Theophylline (1,3-Dimethylxanthine) sodium acetate can be used for asthma and chronic obstructive pulmonary disease (COPD) research[1][2][3][4][5].

IC50 & Target

IL-10

 

IL-6

 

PDE3

 

Human Endogenous Metabolite

 

体外研究
(In Vitro)

Theophylline (1,3-Dimethylxanthine) sodium acetate (1-1000 µM) inhibits cAMP hydrolysis by PDE in homogenates of bronchial tissue to relax human bronchus and pulmonary arteries[1].
Theophylline (1,3-Dimethylxanthine) sodium acetate (10 µg/mL; 24 h; eosinophils) induces apoptosis through a reduction in the antiapoptotic protein Bcl-2[2].
Theophylline (1,3-Dimethylxanthine) sodium acetate (0-500 µM; 2 h; A549 cells) inhibits NF-κB activation, I kappa B alpha (I-κBα) degradation and decreases the level of IL-6 in a concentration-dependent manner[3].
Theophylline (1,3-Dimethylxanthine) sodium acetate (0-1000 µM; 30 min; A549 cells) induces histone deacetylase activity to decrease inflammatory gene expression[4].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Theophylline sodium acetate 相关抗体:

Western Blot Analysis[3]

Cell Line: A549 cells
Concentration: 0, 20, 100 and 500 µM
Incubation Time: 2 hours
Result: Decreased the expression of NF-κB p65 and I-κBα degradation in a concentration-dependent manner.

Western Blot Analysis[2]

Cell Line: Eosinophils
Concentration: 10 µg/mL
Incubation Time: 24 hours
Result: Decreased the expression of Bcl-2.

体内研究
(In Vivo)

Theophylline (1,3-Dimethylxanthine) (100 mg/kg; i.p.; daily, for 9 d; male Swiss mice) has anti-inflammatory activity in mice and increases IL-6 and IL-10 levels and inhibits TNF-α and NO[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Swiss mice[1]
Dosage: 100 mg/kg
Administration: Intraperitoneal injection; daily, for 9 days
Result: Increased IL-6 and IL-10 levels and inhibited TNF-α and NO.

Clinical Trial

分子量

284.18

Formula

C9H10N4Na2O4
CAS 号

8002-89-9
中文名称

乙酸钠茶碱
结构分类
  • Others
初始来源
  • 内源性代谢物
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
Data Sheet (543 KB) 产品使用指南 (1538 KB)

参考文献

  • [1]. Rabe KF, et, al. Theophylline and selective PDE inhibitors as bronchodilators and smooth muscle relaxants. Eur Respir J. 1995 Apr;8(4):637-42.  [Content Brief]

    [2]. Chung IY, et, al. The downregulation of Bcl-2 expression is necessary for theophylline-induced apoptosis of eosinophil. Cell Immunol. 2000 Aug 1;203(2):95-102.  [Content Brief]

    [3]. Ichiyama T, et, al. Theophylline inhibits NF-kappa B activation and I kappa B alpha degradation in human pulmonary epithelial cells. Naunyn Schmiedebergs Arch Pharmacol. 2001 Dec;364(6):558-61.  [Content Brief]

    [4]. Ito K, et, al, Adcock IM, Barnes PJ. A molecular mechanism of action of theophylline: Induction of histone deacetylase activity to decrease inflammatory gene expression. Proc Natl Acad Sci U S A. 2002 Jun 25;99(13):8921-6.  [Content Brief]

    [5]. Barnes PJ. Theophylline. Am J Respir Crit Care Med. 2013 Oct 15;188(8):901-6.  [Content Brief]

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