Z-338 - Cerep

Table 2 Inhibition of Z-338 and ID951551 on the enzyme activities of rCYP
isoforms
Isoforms Inhibitors IC 50 (mol/L) n H
rCYP2C8
(DBF substrate)
Z-338
ID951551
Quercetin
> 100
17
10
1.1
1.4
rCYP2C9
(7-MF substrate)
ID951551
Sulfaphenazole
> 100
0.20 1.1
rCYP3A4
(Testosterone substrate)
ID951551
Sulfaphenazole
21
0.86
1.2
2.3
Effect of Z-338 on the CYP2C8 enzyme activity
1/v
1.4
1.2
1
0.8
0.6
0.4
0.2
0
● DBF 0.25 µM
● DBF 0.5 µM
● DBF 1 µM
● DBF 2 µM
● DBF 2.5 µM
-0.2
-150 -100 -50 0 50 100 150 200 250
Z-338 (M)
Fig. 6 Inhibition of Z-338 on
CYP2C8 activities by
Dixon Plots
Z-338: Ki = 121µM
Quercetin : Ki = 5.8µM