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Theophylline

MCE China：Theophylline

Brand：MedChemExpress (MCE)

Cat. No.HY-B0809

CAS：58-55-9

Synonyms：1,3-Dimethylxanthine; Theo-24

Purity：99.94%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping：Room temperature in continental US; may vary elsewhere.

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

In Vitro：Theophylline (1,3-Dimethylxanthine) (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) (10 µg/mL; 24 h; eosinophils) induces apoptosis through a reduction in the antiapoptotic protein Bcl-2[2]. Theophylline (1,3-Dimethylxanthine) (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) (0-1000 µM; 30 min; A549 cells) induces histone deacetylase activity to decrease inflammatory gene expression[4].

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].

IC50 & Target：IL-10 IL-6 PDE3 Human Endogenous Metabolite

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References：

[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]. Németh ZH, et, al. Amrinone and theophylline differentially regulate cytokine and nitric oxide production in endotoxemic mice. Shock. 1997 May;7(5):371-5.  [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]