Formation of O-demethyl apixaban sulfate in incubations of human liver S9 with SULT inhibitors
Human liver S9 were incubated with 20 or 100 μM O-demethyl apixaban in the presence of PAPS and SULT inhibitors at 37°C for 30 min. Details of the incubation and sample analyses are described under Materials and Methods.
Treatment Group | O-Demethyl Apixaban | Remaining Enzyme Activity |
---|---|---|
μM | % | |
Control | 20 | 100 |
100 | 100 | |
Quercetin (1 μM) | 20 | 0.12 |
100 | 0.54 | |
Estrone (1 μM) | 20 | 90.80 |
100 | 135.36 | |
DCNP (0.5 μM) | 20 | 5.08 |
| 100 | 8.37 |