Relative distribution of radioactivity (%) among various peaks (M1–M9) in the radiochromatographic profiles of untreated, glucuronidase-treated, and DTT-treated 0- to 24-h pooled human urine
| Metabolite | 0–24-h Pooled Human Urine | ||
|---|---|---|---|
| No Treatment | + Glucuronidase | + DTT | |
| Retention time range in min | % Distribution | ||
| M1 (17–18) | 8 | 8 | 7 |
| M2 (19–20) | 44 | 44 | 42 |
| M3 (27–28) | 8 | 8 | —2-a |
| M4 (29–30) | 4 | — | 3 |
| M5 (31–32) | 3 | 3 | 3 |
| M6 (33–34) | 2 | 2 | 1 |
| M7 (34–35) | 3 | 3 | 3 |
| M8 (38–40) | 9 | — | 10 |
| M9 (52–55) | 13 | 23 | 222-b |
| Other | 52-c | 72-d | 82-e |
| Total2-f | 99 | 98 | 99 |
Radioactive peaks are reported as a percentage of the total radioactivity eluted from the column after background subtraction. The recovery of the radioactivity from the column was quantitative.
↵2-a —, percentages less than 1% are not reported.
↵2-b Percentage of radioactivity due to omapatrilat is included in M9 because baseline resolution was not achieved in the radiochromatogram. The relative percentage of radioactivity due to omapatrilat was probably 8 to 9% because M9 accounted for 13% of the radioactivity excreted in the untreated urine, and M3, which was apparently reduced to omapatrilat, accounted for 8%.
↵2-c Two peaks with retention times of 22 to 24 min (3%) and 25 min (2%) are included. These two peaks have not been identified.
↵2-d Two peaks with retention times of 22 to 24 min (3%, unidentified) and 47 min (4%) are included. The peak at 47 min matches with the retention time of BMS-225308 (Fig. 3) and apparently results from glucuronide hydrolysis of M4.
↵2-e Three unidentified peaks with retention times of 22 to 24 min (3%), 25 min (2%), and 37 min (3%) are included.
↵2-f Total is less than 100% because remainder of the radioactivity is distributed in small amounts (<0.5%) in various fractions throughout the radiochromatogram.