| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
| Targets |
Enprofylline targets phosphodiesterases and adenosine receptors. It acts as a competitive nonselective phosphodiesterase inhibitor. It is also a selective and competitive A2B receptor antagonist with a Ki of 7 μM. By inhibiting phosphodiesterase, it increases cAMP levels, leading to bronchodilation. By antagonizing A2B receptors, it may also contribute to its bronchodilator effects.
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| ln Vitro |
N-ethylcarboxamide adenosine (NECA) totally inhibits the release of IL-8 when enprofylline (300 μM) is added [1]. In a concentration-dependent manner, enprofylline (10 μM) suppresses the proliferation caused by NECA (10 μM) [2].
In vitro, enprofylline acts as a selective and competitive A2B receptor antagonist with a Ki of 7 μM. It also acts as a phosphodiesterase inhibitor. Its bronchodilator effects are mediated through these mechanisms. The compound's ability to relax bronchial smooth muscles has been demonstrated in vitro. |
| ln Vivo |
Heart rate (HR) is elevated by enprofenophylline. Male WT mice's HR rose from 529±23 to 590±20 and 562±20 after receiving injections of emprophylline at 7.5 and 30 mg/kg, respectively [3]. While low-dose Enprofylline (7.5 mg/kg) had minimal influence on mice's body temperature, high-dose (30 mg/kg) Enprofylline also decreased the body temperature of female (but not male) WT mice [3].
In vivo, enprofylline improves airflow by relaxing bronchial smooth muscles and reducing airway hyperresponsiveness. It is used for the symptomatic treatment of asthma and chronic obstructive pulmonary disease (COPD). It has also been used in the management of cerebrovascular insufficiency, sickle cell disease, and diabetic neuropathy. |
| Enzyme Assay |
The activity of enprofylline can be assessed using cell-free assays to measure phosphodiesterase inhibition. The enzyme is incubated with its substrate, cAMP, in the presence of varying concentrations of enprofylline. The hydrolysis of cAMP is measured using chromatographic or enzymatic methods. The IC50 for phosphodiesterase inhibition is determined from dose-response curves. Its binding to A2B receptors can be assessed using radioligand binding assays.
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| Cell Assay |
Cell proliferation assay[2]
Cell Types: Human retinal endothelial cells (HREC) Tested Concentrations: 10 μM Incubation Duration: 24, 48, 72 hrs (hours) Experimental Results: NECA (10 μM) induces a time-dependent increase in HREC proliferation (measured by cell counting) , reaching approximately 80% of the cell density after exposure to normal growth medium for 3 days. Emprophylline (10 μM) completely blocked the proliferative effect of NECA when added simultaneously with the analogues. To evaluate the cellular effects of enprofylline, cells expressing A2B receptors or phosphodiesterases are treated with the compound. The inhibition of A2B receptor-mediated signaling or the increase in cAMP levels is measured. The effects on smooth muscle cell relaxation can be assessed in isolated tissue preparations. |
| Animal Protocol |
Animal/Disease Models: A1RKO mice (crossed with C57BL/6 mice for 6 generations) and A2ARKO mice (backcrossed with C57BL/6 mice for more than 10 generations) [3]
Doses: 30 mg/kg Route of Administration: intraperitoneal (ip) injection ( Experimental Results: The HR of male WT mice increased from 529±23 to 590±20 and 562±20 after low dose (7.5 mg/kg) and high dose (30 mg/kg), respectively. In vivo studies with enprofylline typically involve administration to animals or humans via oral or inhalation routes. In models of asthma or COPD, the compound's effects on airway resistance, inflammation, and other parameters are assessed. |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Rapidly absorbed from the digestive tract. Biological Half-Life 1.9 hours. Enprofylline has a molecular formula of C8H10N4O2 and a molecular weight of 194.19. Its CAS number is 41078-02-8. The compound is a xanthine derivative. It is soluble in water and organic solvents. The purity is typically >98%. |
| Toxicity/Toxicokinetics |
Protein Binding
49% Long-term enprofylline administration may be associated with elevation in liver enzyme levels and unpredictable blood levels. As with all xanthine derivatives, it may cause side effects such as nausea, headache, and insomnia. It should be used under medical supervision. |
| References |
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| Additional Infomation |
Enprophylline is a xanthine compound with a propyl substituent at the 3-position. It is a bronchodilator used to treat symptoms of asthma and chronic obstructive pulmonary disease (COPD), as well as cerebrovascular insufficiency, sickle cell disease, and diabetic neuropathy. It has multiple effects as a nonsteroidal anti-inflammatory drug (NSAID), bronchodilator, anti-asthmatic, and antiarrhythmic. Enprophylline is a derivative of theophylline and has similar bronchodilatory properties. Enprophylline is used to treat asthma, COPD, cerebrovascular insufficiency, sickle cell disease, and diabetic neuropathy. Long-term use of enprophylline may lead to elevated liver enzyme levels and fluctuations in blood drug concentration. Drug Indications: Used to treat asthma symptoms. Also used to treat peripheral vascular disease, as well as cerebrovascular insufficiency, sickle cell disease, and diabetic neuropathy. Mechanism of Action: Enprophylline inhibits erythrocyte phosphodiesterase, leading to increased erythrocyte cAMP activity. Subsequently, the deformability of the erythrocyte membrane is enhanced. In addition to enhancing erythrocyte activity, entrobelcin can also reduce blood viscosity by lowering plasma fibrinogen concentration and enhancing fibrinolytic activity.
Pharmacodynamics Entrobelcin is a synthetic dimethylxanthine derivative with a structure related to theophylline and caffeine. It antagonizes erythrocyte phosphodiesterase, thereby increasing cAMP activity. Enprofylline is a xanthine derivative used as a bronchodilator in the treatment of asthma and COPD. It acts as a phosphodiesterase inhibitor and an A2B receptor antagonist. It is a valuable compound in pharmacological research on respiratory and adenosine-mediated pathophysiological mechanisms. |
| Molecular Formula |
C8H10N4O2
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| Molecular Weight |
194.19
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| Exact Mass |
194.08
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| CAS # |
41078-02-8
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| PubChem CID |
1676
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| Appearance |
White to light yellow solid powder
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| Density |
1.367 g/cm3
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| Melting Point |
287-289 °C
287 - 289 °C |
| Index of Refraction |
1.583
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| LogP |
0.3
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
14
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| Complexity |
268
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
SIQPXVQCUCHWDI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C8H10N4O2/c1-2-3-12-6-5(9-4-10-6)7(13)11-8(12)14/h4H,2-3H2,1H3,(H,9,10)(H,11,13,14)
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| Chemical Name |
3-propyl-7H-purine-2,6-dione
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| Synonyms |
3-propylxanthineEnprofylline 3-n-Propylxanthine Enprofyllinum3-Propylxanthine Enprofilina enprofylline
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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) |
DMSO : ~62.5 mg/mL (~321.85 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (10.71 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 20.8 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. Solubility in Formulation 2: ≥ 2.08 mg/mL (10.71 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 5.1496 mL | 25.7480 mL | 51.4960 mL | |
| 5 mM | 1.0299 mL | 5.1496 mL | 10.2992 mL | |
| 10 mM | 0.5150 mL | 2.5748 mL | 5.1496 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.
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