8-HYDROXYWARFARIN

8-HYDROXYWARFARIN Structure
8-HYDROXYWARFARIN structure
Common Name 8-HYDROXYWARFARIN
CAS Number 17834-04-7 Molecular Weight 324.32700
Density 1.384g/cm3 Boiling Point 519.6ºC at 760mmHg
Molecular Formula C19H16O5 Melting Point 185-187ºC
MSDS Chinese USA Flash Point 189.3ºC
Symbol GHS07
GHS07
Signal Word Warning

Investigation of two-dimensional high performance liquid chromatography approaches for reversed phase resolution of warfarin and hydroxywarfarin isomers.

J. Chromatogr. A. 1363 , 200-6, (2014)

Several offline and online 2D HPLC methods were investigated for the reversed phase resolution of a complex mixture of closely related warfarin and hydroxywarfarin isomers. By combining reversed phase achiral/chiral HPLC separation with UV-triggered fraction ...

Hydroxywarfarin metabolites potently inhibit CYP2C9 metabolism of S-warfarin.

Chem. Res. Toxicol. 23(5) , 939-45, (2010)

Coumadin (R/S-warfarin) anticoagulant therapy poses a risk to over 50 million Americans, in part due to interpersonal variation in drug metabolism. Consequently, it is important to understand how metabolic capacity is influenced among patients. Cytochrome P45...

Metabolism of R- and S-warfarin by CYP2C19 into four hydroxywarfarins.

Drug Metab. Lett. 6(3) , 157-64, (2012)

Coumadin (R/S-warfarin) is a highly efficacious and widely used anticoagulant; however, its highly variable metabolism remains an important contributor to uncertainties in therapeutic responses. Pharmacogenetic studies report conflicting findings on the clini...

Warfarin is an effective modifier of multiple UDP-glucuronosyltransferase enzymes: evaluation of its potential to alter the pharmacokinetics of zidovudine.

J. Pharm. Sci. 104(1) , 244-56, (2014)

In this study, we aimed to determine the modulatory effects of warfarin (an extensively used anticoagulant drug) and its metabolites on UDP-glucuronosyltransferase (UGT) activity and to assess the potential of warfarin to alter the pharmacokinetics of zidovud...

Analysis of R- and S-hydroxywarfarin glucuronidation catalyzed by human liver microsomes and recombinant UDP-glucuronosyltransferases.

J. Pharmacol. Exp. Ther. 340(1) , 46-55, (2012)

Coumadin (R-, S-warfarin) is a challenging drug to accurately dose, both initially and for maintenance, because of its narrow therapeutic range and wide interpatient variability and is typically administered as a racemic (Rac) mixture, which complicates the b...

Identification of hydroxywarfarin binding site in human UDP glucuronosyltransferase 1a10: phenylalanine90 is crucial for the glucuronidation of 6- and 7-hydroxywarfarin but not 8-hydroxywarfarin.

Drug Metab. Dispos. 36(11) , 2211-8, (2008)

Recent studies show that the extrahepatic human UDP-glucuronosyltransferase (UGT)1A10 is capable of phase II glucuronidation of several major cytochrome P450 metabolites of warfarin (i.e., 6-, 7-, and 8-hydroxywarfarin). This study expands on this finding by ...

Formation of (R)-8-hydroxywarfarin in human liver microsomes. A new metabolic marker for the (S)-mephenytoin hydroxylase, P4502C19.

Drug Metab. Dispos. 24(5) , 610-4, (1996)

Kinetic studies demonstrate that two forms of human liver cytochrome P450 are responsible for the formation of (R)-8-hydroxywarfarin: a low-affinity enzyme (KM approximately 1.5 mM), previously identified as P4501A2; and a high-affinity enzyme (KM = 330 micro...

Responsiveness to low-dose warfarin associated with genetic variants of VKORC1, CYP2C9, CYP2C19, and CYP4F2 in an Indonesian population.

Eur. J. Clin. Pharmacol. 69(3) , 395-405, (2013)

The aim of this study was to assess the pharmacokinetics and pharmacodynamics of warfarin associated with genetic polymorphisms in VKORC1, CYP2C9, CYP2C19, and CYP4F2 in Indonesian patients treated with low-dose warfarin.Genotyping of VKORC1, CYP2C9, CYP2C19,...

Prediction of human disposition toward S-3H-warfarin using chimeric mice with humanized liver.

Drug Metab. Pharmacokinet. 24(2) , 153-60, (2009)

Chimeric mice, constructed by transplanting human hepatocytes, are useful for predicting the human metabolism of drug candidates. In this study, we investigated whether these mice show similar metabolic profile to humans by examining the hydroxylation of S-wa...

Chromatographic resolution of closely related species: separation of warfarin and hydroxylated isomers. Regalado, E. L., et al., doi:10.1016/j.chroma.2013.07.092

J. Chromatogr. A. , (2013)