Theophylline monohydrate
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Theophylline (1,3-Dimethylxanthine) monohydrate is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline (1,3-Dimethylxanthine) monohydrate inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) monohydrate has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) monohydrate induces apoptosis. Theophylline (1,3-Dimethylxanthine) monohydrate can be used for asthma and chronic obstructive pulmonary disease (COPD) research.
For research use only. We do not sell to patients.
- Purity: 99.93%
- CAS No.: 5967-84-0
- Formula: C7H10N4O3
- Molecular Weight:198.18
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
All Adenosine Receptor Isoforms
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Biological Activity
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IL-10 |
IL-6 |
PDE3 |
Theophylline (1,3-Dimethylxanthine) monohydrate (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) monohydrate (10 μg/mL; 24 h; eosinophils) induces apoptosis through a reduction in the antiapoptotic protein Bcl-2[2].
Theophylline (1,3-Dimethylxanthine) monohydrate (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) monohydrate (0-1000 μM; 30 min; A549 cells) induces histone deacetylase activity to decrease inflammatory gene expression[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549 cells
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Concentration:0, 20, 100 and 500 µM
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Incubation Time:2 hours
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Result:Decreased the expression of NF-κB p65 and I-κBα degradation in a concentration-dependent manner.
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Cell Line:Eosinophils
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Concentration:10 µg/mL
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Incubation Time:24 hours
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Result:Decreased the expression of Bcl-2.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Swiss mice[1]
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Dosage:100 mg/kg
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Administration:Intraperitoneal injection; daily, for 9 days
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Result:Increased IL-6 and IL-10 levels and inhibited TNF-α and NO.
Chemical Information
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CAS No. 5967-84-0
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Appearance Solid
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Molecular Weight 198.18
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Formula C7H10N4O3
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Color White to off-white
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SMILES
O=C1C2=C(N(C)C(N1C)=O)N=CN2.O
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Synonyms
1,3-Dimethylxanthine monohydrate; Theo-24 monohydrate
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Purity & Documentation
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Data Sheet (277 KB)
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SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
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Handling Instructions (2659 KB)
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]. 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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)