Formation of irosustat metabolites in incubations with human cDNA-expressed P450s and FMO3 enzyme
Results are expressed as means of metabolite peak area units from duplicate incubations.
| Enzyme | Mean Peak Area | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| M7 | M8 | M9 | M11 | M13 | M14 | M16 | M18 | P-36 | |
| CYP1A1 | 3784 | N.D. | N.D. | N.D. | 25,693 | 30,242 | 30,049 | 3196 | N.D. |
| CYP1A2 | 39,779 | 8781 | 15849 | N.D. | 105,131 | 69,618 | 37,042 | 16,618 | N.D. |
| CYP1B1 | N.D. | N.D. | N.D. | N.D. | 4978 | N.D. | 15,681 | N.D. | N.D. |
| CYP2A6 | N.D. | N.D. | N.D. | N.D. | N.D. | N.D. | N.D. | N.D. | N.D. |
| CYP2B6 | N.D. | N.D. | N.D. | N.D. | N.D. | N.D. | 3132 | N.D. | 5565 |
| CYP2C8 | N.D. | N.D. | 2653 | N.D. | 2731 | N.D. | N.D. | N.D. | N.D. |
| CYP2C9 | 4129 | N.D. | N.D. | N.D. | 4904 | N.D. | 2106 | 2648 | N.D. |
| CYP2C19 | 15,105 | 4528 | 2444 | N.D. | 22,693 | N.D. | 14,730 | 6638 | 8235 |
| CYP2D6 | 125,154 | 20,891 | 3785 | N.D. | 52,889 | N.D. | 12,864 | 4213 | N.D. |
| CYP2E1 | 10,210 | 1923 | N.D. | N.D. | 2599 | N.D. | N.D. | N.D. | N.D. |
| CYP3A4 | N.D. | N.D. | 7425 | N.D. | 88,686 | 51,656 | 26,628 | 5335 | N.D. |
| CYP3A5 | 1855 | N.D. | 2159 | N.D. | 12,175 | 1915 | 4855 | 2915 | N.D. |
| FMO3 | N.D. | N.D. | N.D. | N.D. | N.D. | N.D. | N.D. | N.D. | N.D. |
N.D., not detected.