Furafylline

Names

[ Name ]:
Furafylline

[Synonym ]:
1H-Purine-2,6-dione, 3-(2-furanylmethyl)-3,7-dihydro-1,8-dimethyl-
3-(2-Furylmethyl)-1,8-dimethyl-3,7-dihydro-1H-purine-2,6-dione
furafylline
3-Furfuryl-1,8-dimethylxanthine
3-(furan-2-ylmethyl)-1,8-dimethyl-3,7-dihydro-1H-purine-2,6-dione

Biological Activity

[Description]:

Furafylline is a potent and selective inhibitor of human cytochrome P450IA2 with an IC50 of 0.07 μM.

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> Cytochrome P450

Research Areas >> Cancer

[Target]

IC50: 0.07 μM (human cytochrome P450IA2)[1]

[In Vivo]

Furafylline is a potent and selective inhibitor of human cytochrome P450IA2 with an IC50 of 0.07 μM in kinase experiment. Furafylline is a methylxanthine derivative that is introduced as a long-acting replacement for theophylline in the treatment of asthma. Administration of Furafylline is associated with an elevation in plasma levels of caffeine, due to inhibition of caffeine oxidation, a reaction catalysed by one or more hydrocarbon-inducible isoenzymes of P450. Furafylline has either very little or no effect on human monooxygenase activities catalysed by other isoenzymes of P450, including P4501ID1, P4501IC, P450IIIA[1].

[References]

[1]. Sesardic D, et al. Furafylline is a potent and selective inhibitor of cytochrome P450IA2 in man. Br J Clin Pharmacol. 1990 Jun;29(6):651-63.

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
543.6±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C₁₂H₁₂N₄O₃

[ Molecular Weight ]:
260.249

[ Flash Point ]:
282.6±32.9 °C

[ Exact Mass ]:
260.090942

[ PSA ]:
85.82000

[ LogP ]:
-0.24

[ Vapour Pressure ]:
0.0±1.5 mmHg at 25°C

[ Index of Refraction ]:
1.637

[ Storage condition ]:
2-8℃

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ RIDADR ]:
NONH for all modes of transport

[ WGK Germany ]:
3

[ HS Code ]:
2939590000

Customs

[ HS Code ]: 2939590000

Articles

Physicochemical and drug metabolism characterization of a series of 4-aminoquinoline-3-hydroxypyridin-4-one hybrid molecules with antimalarial activity.

Expert Opin. Drug Metab. Toxicol. 10(10) , 1313-24, (2014)

Drug resistance by Plasmodium falciparum remains a challenge in malaria chemotherapy. This paper will focus on physicochemical and drug metabolism characterization of a series of 4-aminoquinoline-3-hy...

The cytochrome P450-catalyzed metabolism of levomepromazine: a phenothiazine neuroleptic with a wide spectrum of clinical application.

Biochem. Pharmacol. 90(2) , 188-95, (2014)

The aim of the present study was to identify cytochrome P450 isoenzymes (CYPs) involved in the 5-sulfoxidation and N-demethylation of the aliphatic-type phenothiazine neuroleptic levomepromazine in hu...

Identification of the human cytochrome P450 enzymes involved in the two oxidative steps in the bioactivation of clopidogrel to its pharmacologically active metabolite.

Drug Metab. Dispos. 38(1) , 92-9, (2010)

The aim of the current study is to identify the human cytochrome P450 (P450) isoforms involved in the two oxidative steps in the bioactivation of clopidogrel to its pharmacologically active metabolite...