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Effect of chemical modification of the linker X on activity profiles
 |
||||
|---|---|---|---|---|
| Compds | X | C3 Configuration (3R and/or 3S) |
IC50 (nM) Ca assay |
Stability in rat liver microsomesa remaining% |
| 29 |  |
(3S) | 170 | 38 |
| 30 |  |
(3S) | 86 | 19 |
| 31 |  |
(3S) | 81 | 23 |
| 32 |  |
(3S) | 57 | 29 |
| 1a |  |
(3RS) | 28 | 33 |
The data show the remaining% 15 min after incubating with the 0.5 mg/mL rat liver microsomes.
