Relative distribution (percentage of sample) of radioactive metabolites in incubation of [14C]muraglitazar with hepatocytes from mice, rats, monkeys, and humans
Metabolitea | Distribution of Metabolites in Hepatocyte Incubationsb | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Control | Mouse | Rat | Monkey | Human | |||||
| % | |||||||||
| M1 | 9.5 | 23.6 | 12 | 7.6 | 5.7 | ||||
| M2 | N.D.c | 4.8 | trace | trace | trace | ||||
| M3 | N.D. | 0.3 | trace | N.D. | trace | ||||
| M5 | N.D. | 3.0 | trace | trace | trace | ||||
| M6 | N.D. | 0.3 | trace | 11 | 1.6 | ||||
| M7 | N.D. | 1.2 | trace | 0.5 | trace | ||||
| M8 | N.D. | 0.8 | 0.3 | trace | 0.2 | ||||
| M8a | N.D. | 0.3 | trace | trace | trace | ||||
| M10 | 1.0 | 11 | 1.3 | 0.8 | 1.9 | ||||
| M11 | N.D. | 5.4 | 2.0 | 7.9 | 4.4 | ||||
| M12 | N.D. | 0.8 | trace | 13 | 0.9 | ||||
| M13 | N.D. | 5.2 | 0.5 | 1.7 | 1.1 | ||||
| M14 | N.D. | 1.3 | 0.3 | 0.6 | 0.5 | ||||
| M15 | N.D. | 1.2 | 2.2 | 2.1 | 2.3 | ||||
| M17b | N.D. | traced | trace | trace | trace | ||||
| M18a/be | N.D. | 2.7 | 0.5 | 2.8 | 0.2 | ||||
| M20 | N.D. | trace | trace | trace | trace | ||||
| M21 | N.D. | 5.7 | 0.3 | trace | trace | ||||
| M22 | 3.5 | 1.4 | 7.5 | 1.3 | 4.5 | ||||
| Parent | 83 | 20 | 69 | 44 | 73 | ||||
| Otherf | 0.5 | 6.1 | 1.5 | 1.7 | 0.5 | ||||
| Totalg | 97 | 95 | 97 | 95 | 96 | ||||
↵ a Metabolites are assigned based on retention times of radioactive peaks and LC/MS analysis.
↵ b Metabolites are reported as a percentage of the total radioactivity eluted from the column.
↵ c N.D., not detectable by LC/MS.
↵ d trace = <0.2% radioactivity and detectable by LC/MS.
↵ e M18a/b contained a and b isomers in approximately the same amounts.
↵ f Other = unidentified peaks.
↵ g Total is less than 100% because the remainder of the radioactivity is distributed in small amounts (<0.2%) in various fractions throughout the radiochromatogram.