The inhibition of diclofenac hydroxylation (CYP2C9) by SKF525A derivatives in human liver microsomes NADPH-fortified human liver microsomes (1 mg/ml of a mix of six commercial preparations) were incubated with diclofenac (50 μM), and the concentrations of the inhibitors are indicated. Each value is the mean of two independent incubations with the superscript indicating the ±range (to the nearest integer).
Inhibitor | Inhibition at Inhibitor Concentration [μM] | IC50a | ||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 0.52 | 2.06 | 4.13 | 8.25 | 16.5 | 33 | 100 | ||||||||
| % | % | % | % | % | % | % | μM | |||||||
| SKF-Acid | 102 | 342 | 483 | 642 | 861 | 941 | ∼4 | |||||||
| SKF-Alcohol | 32 | 54 | 160 | 521 | 841 | ∼33 | ||||||||
| SKF26754 | 152 | 384 | 451 | 743 | 33–100 | |||||||||
| SKF8742 | 171 | 202 | 443 | >100 | ||||||||||
| SKF525A |
|
|
|
| 130 | 254 | 444 | >100 | ||||||
↵ a The IC50 value was estimated by interpolation