Size | Price | Stock | Qty |
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500mg |
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5g |
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Other Sizes |
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ln Vitro |
Human bronchial and pulmonary arteries are relaxed when theophylline (1,3-dimethylxanthine) (1-1000 µM) inhibits PDE-induced cAMP hydrolysis in bronchial tissue homogenates [1]. By decreasing the anti-apoptotic protein Bcl-2, theophylline (1,3-dimethylxanthine) (10 µg/mL; 24 hours; eosinophils) promotes apoptosis [2]. In A549 cells, theophylline (1,3-dimethylxanthine) (0-500 µM; 2 hours) suppresses the activation of NF-κB, the degradation of I-κBα, and the production of IL-6[3]. Histone deacetylase activity is induced by theophylline (1,3-dimethylxanthine) (0-1000 µM; 30 min; A549 cells), which lowers the expression of inflammatory genes [4].
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ln Vivo |
In male Swiss mice, theophylline (1,3-dimethylxanthine) (100 mg/kg; i.p.; daily for 9 days) shows anti-inflammatory effect by raising IL-6 and IL-10 levels and suppressing NO and TNF-α [1].
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Cell Assay |
Western Blot Analysis [3]
Cell Types: A549 Cell Tested Concentrations: 0, 20, 100 and 500 µM Incubation Duration: 2 hrs (hours) Experimental Results: diminished NF-κB p65 expression and I-κBα degradation in a concentration-dependent manner. Western Blot Analysis[2] Cell Types: Eosinophils Tested Concentrations: 10 µg/mL Incubation Duration: 24 hrs (hours) Experimental Results: diminished Bcl-2 expression. |
Animal Protocol |
Animal/Disease Models: Male Swiss mice [1]
Doses: 100 mg/kg Route of Administration: intraperitoneal (ip) injection; one time/day for 9 days Experimental Results: Increased IL-6 and IL-10 levels and inhibited TNF-α and NO. |
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.
[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. [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. [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. [5]. Barnes PJ. Theophylline. Am J Respir Crit Care Med. 2013 Oct 15;188(8):901-6. |
Molecular Formula |
C7H8N4O2
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Molecular Weight |
180.1640
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CAS # |
58-55-9
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Related CAS # |
Theophylline-d6;117490-39-8;Theophylline sodium glycinate;8000-10-0;Theophylline monohydrate;5967-84-0;Theophylline sodium acetate;8002-89-9
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SMILES |
O=C1C2=C(N=C([H])N2[H])N(C([H])([H])[H])C(N1C([H])([H])[H])=O
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
0.1 M NaOH : ~20 mg/mL (~111.01 mM)
DMSO : ~11.11 mg/mL (~61.67 mM) H2O : ~5 mg/mL (~27.75 mM) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.11 mg/mL (6.16 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 11.1 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.11 mg/mL (6.16 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 11.1 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1.11 mg/mL (6.16 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 11 mg/mL (61.06 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 5.5506 mL | 27.7531 mL | 55.5062 mL | |
5 mM | 1.1101 mL | 5.5506 mL | 11.1012 mL | |
10 mM | 0.5551 mL | 2.7753 mL | 5.5506 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.