FurafyllineAn inhibitor of Cytochrome P450 (CYP1A2) and phosphodiesterase (PDE)

Furafylline (CAS 80288-49-9)

Furafylline | CAS 80288-49-9 is rated 5.0 out of 5 by 1.
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Synonym: 3-(2-Furanylmethyl)-3,7-dihydro-1,8-dimethyl-1H-purine-2,6-dione
Application: An inhibitor of Cytochrome P450 (CYP1A2) and phosphodiesterase (PDE)
CAS Number: 80288-49-9
Purity: ≥95%
Molecular Weight: 260.25
Molecular Formula: C12H12N4O3
* Refer to Certificate of Analysis for lot specific data (including water content).
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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.


References

1. Boulenc, X., et al., 1992. Regulation of cytochrome P450IA1 gene expression in a human intestinal cell line, Caco-2. The Journal of pharmacology and experimental therapeutics. 263(3): 1471-8. PMID: 1469646
2. Sesardic, D., et al., 1990. Furafylline is a potent and selective inhibitor of cytochrome P450IA2 in man. British journal of clinical pharmacology. 29(6): 651-63. PMID: 2378786
3. Segura, J., et al., 1986. Some pharmacokinetic characteristics of furafylline, a new 1,3,8-trisubstituted xanthine. The Journal of pharmacy and pharmacology. 38(8): 615-8. PMID: 2876080

Physical State :
Solid
Solubility :
Soluble in ethanol (0.33 mg/ml), and DMSO (>10 mg/mL). Insoluble in water.
Storage :
Store at room temperature
Melting Point :
274-275° C
Refractive Index :
n20D 1.64 (Predicted)
IC50 :
Cytochrome P450 1A2: IC50 = 2419 nM (human)
Ki Data :
Cytochrome P450 1A2: Ki= 3 µM (human)
pK Values :
pKa: 9.07, pKb: 2.4
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
3433
MDL Number :
MFCD00153799
SMILES :
CC1=NC2=C(N1)C(=O)N(C(=O)N2CC3=CC=CO3)C

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Certificate of Analysis

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Furafylline  Product Citations

See how others have used Furafylline. Click on the entry to view the PubMed entry .

Citations 1 to 2 of 2 total

PMID: # 26174047  Feng, R. et al. 2015. Scientific reports. 5: 12155.

PMID: # 25422175  Wang, W. et al. 2015. Chirality. 27: 170-6.

Citations 1 to 2 of 2 total
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Rated 5 out of 5 by from Sesardic et al Sesardic et al. (PubMed ID 2378786) found that furafylline was a potent and selective cytochrome P450IA2 in the human liver. -SCBT Publication Review
Date published: 2015-02-07
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