| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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Enprofylline, a xanthine analogue, is a potent and competitive A2B receptor antagonist and phosphodiesterase inhibitor used in the treatment of asthma as a bronchodilator. Enprofylline is used in asthma, chronic obstructive pulmonary disease, and in the management of cerebrovascular insufficiency, sickle cell disease, and diabetic neuropathy. Long-term enprofylline administration may be associated with elevation in liver enzyme levels and unpredictable blood levels.
| 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].
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| 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].
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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. |
| 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. |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Rapidly absorbed from the digestive tract Biological Half-Life 1.9 hours |
| Toxicity/Toxicokinetics |
Protein Binding
49% |
| References |
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| Additional Infomation |
Enprofylline is xanthine bearing a propyl substituent at position 3. A bronchodilator, it is used for the symptomatic treatment of asthma and chronic obstructive pulmonary disease, and in the management of cerebrovascular insufficiency, sickle cell disease, and diabetic neuropathy. It has a role as a non-steroidal anti-inflammatory drug, a bronchodilator agent, an anti-asthmatic drug and an anti-arrhythmia drug.
Enprofylline is a derivative of theophylline which shares bronchodilator properties. Enprofylline is used in asthma, chronic obstructive pulmonary disease, and in the management of cerebrovascular insufficiency, sickle cell disease, and diabetic neuropathy. Long-term enprofylline administration may be associated with elevation in liver enzyme levels and unpredictable blood levels. Drug Indication Used in the management of symptoms of asthma. Also used in the treatment of peripheral vascular diseases and in the management of cerebrovascular insufficiency, sickle cell disease, and diabetic neuropathy. Mechanism of Action Enprofylline inhibits erythrocyte phosphodiesterase, resulting in an increase in erythrocyte cAMP activity. Subsequently, the erythrocyte membrane becomes more resistant to deformity. Along with erythrocyte activity, enprofylline also decreases blood viscosity by reducing plasma fibrinogen concentrations and increasing fibrinolytic activity. Pharmacodynamics Enprofylline is a synthetic dimethylxanthine derivative structurally related to theophylline and caffeine. It antagonizes erythrocyte phosphodiesterase, increasing cAMP activity. |
| 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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