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Furafylline, a methylxanthine derivative, is a potent inhibitor of human cytochrome P450IA2 (CYP1A2) and phosphodiesterase (PDE). It was introduced in hope of being a long-acting replacement for theophylline in the treatment of asthma.
| ln Vivo |
Furafylline, with an IC50 of 0.07 μM in kinase tests, is a strong and specific inhibitor of human cytochrome P450IA2. A methylxanthine derivative called furafylline is used to treat asthma in place of theophylline, providing a longer-acting option. When furafylline is administered, the inhibition of caffeine oxidation—a process that is performed by P450 isoenzymes and is caused by one or more hydrocarbons—may lead to an increase in plasma caffeine levels. When human monooxygenase is catalyzed by different P450 isoenzymes, such as P4501ID1, P4501IC, and P450IIIA, furafylline has little to no effect on its activity [1].
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| ADME/Pharmacokinetics |
Metabolism / Metabolites
Furafylline has known human metabolites that include 3-[(furan-2-yl)methyl]-8-hydroxy-1-methyl-2,3,6,7-tetrahydro-1H-purine-2,6-dione. |
| References | |
| Additional Infomation |
Furafylline is an oxopurine.
Furafylline is a derivative of methylxanthine derivative. It was developed on the context of asthma as a long-acting alternative for [theophylline]. |
| Molecular Formula |
C12H12N4O3
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|---|---|
| Molecular Weight |
260.24900
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| Exact Mass |
260.09
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| CAS # |
80288-49-9
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| PubChem CID |
3433
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| Appearance |
White to light yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
543.6±60.0 °C at 760 mmHg
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| Flash Point |
282.6±32.9 °C
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| Vapour Pressure |
0.0±1.5 mmHg at 25°C
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| Index of Refraction |
1.637
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| LogP |
-0.24
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
19
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| Complexity |
402
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
KGQZGCIVHYLPBH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H12N4O3/c1-7-13-9-10(14-7)16(6-8-4-3-5-19-8)12(18)15(2)11(9)17/h3-5H,6H2,1-2H3,(H,13,14)
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| Chemical Name |
3-(furan-2-ylmethyl)-1,8-dimethyl-7H-purine-2,6-dione
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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 |
| 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 : ~12.5 mg/mL (~48.03 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.17 mg/mL (8.34 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 21.7 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: ≥ 2.17 mg/mL (8.34 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 21.7 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 | 3.8425 mL | 19.2123 mL | 38.4246 mL | |
| 5 mM | 0.7685 mL | 3.8425 mL | 7.6849 mL | |
| 10 mM | 0.3842 mL | 1.9212 mL | 3.8425 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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