Date published: 2025-10-19

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Furafylline (CAS 80288-49-9)

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Alternate Names:
3-(2-Furanylmethyl)-3,7-dihydro-1,8-dimethyl-1H-purine-2,6-dione
Application:
Furafylline is an inhibitor of Cytochrome P450 (CYP1A2) and phosphodiesterase (PDE)
CAS Number:
80288-49-9
Purity:
≥95%
Molecular Weight:
260.25
Molecular Formula:
C12H12N4O3
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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Furafylline is a methyl xanthine derivative with an expanded duration of action than that of theophylline. Furafylline acts as an inhibitor of CYP1A2 (cytochrome p450) and PDE (phosphodiesterase). Inhibition of CYP has the effect of slowing oxidative metabolism of xenobiotics, while inhibition of PDE prevents the hydrolysis of secondary messenger molecules, which in turn prolongs signal transduction and enhances its effects.


Furafylline (CAS 80288-49-9) References

  1. Regulation of cytochrome P450IA1 gene expression in a human intestinal cell line, Caco-2.  |  Boulenc, X., et al. 1992. J Pharmacol Exp Ther. 263: 1471-8. PMID: 1469646
  2. Furafylline is a potent and selective inhibitor of cytochrome P450IA2 in man.  |  Sesardic, D., et al. 1990. Br J Clin Pharmacol. 29: 651-63. PMID: 2378786
  3. Improvement of the chemical inhibition phenotyping assay by cross-reactivity correction.  |  Njuguna, NM., et al. 2016. Drug Metab Pers Ther. 31: 221-228. PMID: 27718490
  4. Candidate cytochrome P450 genes for ethoxyresorufin O-deethylase activity in oyster Crassostrea gigas.  |  Siebert, MN., et al. 2017. Aquat Toxicol. 189: 142-149. PMID: 28623690
  5. Some pharmacokinetic characteristics of furafylline, a new 1,3,8-trisubstituted xanthine.  |  Segura, J., et al. 1986. J Pharm Pharmacol. 38: 615-8. PMID: 2876080
  6. Study on the inhibitory effect of furafylline and troleandomycin in the 7-methoxyresorufin-O-demethylase and nifedipine oxidase activities in hepatic microsomes from four poultry species using high-performance liquid chromatography coupled with fluorescence and ultraviolet detection.  |  Murcia, H., et al. 2019. J Pharm Biomed Anal. 164: 148-154. PMID: 30390556
  7. Interspecies Variation in NCMN-O-Demethylation in Liver Microsomes from Various Species.  |  Dai, Z., et al. 2019. Molecules. 24: PMID: 31366067
  8. Roles of human cytochrome P450 1A2 in coumarin 3,4-epoxidation mediated by untreated hepatocytes and by those metabolically inactivated with furafylline in previously transplanted chimeric mice.  |  Miura, T., et al. 2021. J Toxicol Sci. 46: 525-530. PMID: 34719555
  9. Interindividual Variability in Cytochrome P450 3A and 1A Activity Influences Sunitinib Metabolism and Bioactivation.  |  Burnham, EA., et al. 2022. Chem Res Toxicol. 35: 792-806. PMID: 35484684
  10. Cytochrome P450 inhibition activities of non-standardized botanical products.  |  Abduraman, MA., et al. 2022. J Ethnopharmacol. 296: 115406. PMID: 35659627
  11. Defining the Selectivity of Chemical Inhibitors Used for Cytochrome P450 Reaction Phenotyping: Overcoming Selectivity Limitations with a Six-Parameter Inhibition Curve-Fitting Approach.  |  Doran, AC., et al. 2022. Drug Metab Dispos.. PMID: 35777846
  12. Characterization of the inhibition of P4501A2 by furafylline.  |  Clarke, SE., et al. 1994. Xenobiotica. 24: 517-26. PMID: 7975717
  13. Isoform-selective mechanism-based inhibition of human cytochrome P450 1A2 by furafylline.  |  Kunze, KL. and Trager, WF. 1993. Chem Res Toxicol. 6: 649-56. PMID: 8292742

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

Furafylline, 5 mg

sc-215061
5 mg
$294.00