TABLE 2

Inhibition of KTZ on APZ metabolite formation in liver and small intestinal microsomes from humans and cynomolgus monkeys

Activity was measured at a substrate concentration of 100 μM. IC50 values are calculated for duplicate incubations.

MetaboliteIC50
Liver MicrosomesIntestinal Microsomes
HumanMonkeyHumanMonkey
μM
1′-OH APZ0.0710.0860.0270.018
4-OH APZ0.0350.0690.0260.017