Literature summary for 3.4.21.6 extracted from

Zhang, D.; He, K.; Raghavan, N.; Wang, L.; Crain, E.J.; He, B.; Xin, B.; Luettgen, J.M.; Wong, P.C.
Metabolism, pharmacokinetics and pharmacodynamics of the factor Xa inhibitor apixaban in rabbits (2010), J. Thromb. Thrombolysis, 29, 70-80.

Search for more literature for 3.4.21.6

Inhibitors

Inhibitors	Comment	Organism	Structure
apixaban	i.e. BMS-562247 or 1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-1-yl)phenyl]-4,5-dihydropyrazolo[5,4-c]pyridine-3-carboxamide. Metabolism, pharmacokinetics and pharmacodynamics of the factor Xa inhibitor apixaban. Oxidative metabolism of radiolabeled apixaban by liver microsomes is approximately 20times faster in rabbits than in rats or humans. Prominant metabolites are O-demethyl apixaban, O-demethyl apixaban glucuronide and O-demethyl apixaban sulfate, metabolic profiles, overview	Oryctolagus cuniculus

Localization

Localization	Comment	Organism	GeneOntology No.	Textmining
microsome	-	Oryctolagus cuniculus	-	-

Organism

Organism	UniProt	Comment	Textmining
Oryctolagus cuniculus	-	-	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
blood plasma	-	Oryctolagus cuniculus	-
liver	-	Oryctolagus cuniculus	-

Synonyms

Synonyms	Comment	Organism
factor Xa	-	Oryctolagus cuniculus
FXa	-	Oryctolagus cuniculus

Temperature Optimum [°C]

Temperature Optimum [°C]	Temperature Optimum Maximum [°C]	Comment	Organism
37	-	assay at	Oryctolagus cuniculus

pH Optimum

pH Optimum Minimum	pH Optimum Maximum	Comment	Organism
7.8	-	assay at	Oryctolagus cuniculus

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.00022	-	inhibition of FXa activity ex vivo	Oryctolagus cuniculus	apixaban

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Release 2023.1 (January 2023)