Comparison of pharmacological activity (IC50 MS) and kinetic parameters (Ki app) of CHL derivatives
| Compound | IC50 MSMicrosomes | Ki app | |
|---|---|---|---|
| Hepatocytes | Oatp 1 | ||
| μM | μM | μM | |
| S 1743 | 0.085 ± 0.01 | 1.1 ± 0.2 | 0.9 ± 0.3 |
| S 4048 | 0.004 ± 0.001 | 2.1 ± 0.6 | 0.9 ± 0.3 |
| S 3483 | 0.21 ± 0.04 | 2.1 ± 0.8 | 4.6 ± 2.1 |
| S 0727 | 90 ± 4 | 1.2 ± 0.3 | 3.2 ± 0.9 |
| S 7132 | 7.1 ± 1.1 | 4.3 ± 0.9 | 3.9 ± 0.9 |
| S 1398 | >100 | 11 ± 7 | 7.3 ± 2.4 |
| S 3025 | 0.026 ± 0.025 | 2.8 ± 0.8 | 6.4 ± 3.3 |
| Chlorogenic acid | >100 | >100 | >100 |
Pharmacological activity of CHL derivatives was determined by measuring Gl-6-Pase activity in the presence of different CHL derivatives in rat liver microsomes and is expressed as IC50 values. Apparent inhibition constants (Ki app) of CHL derivatives were determined in freshly isolated rat hepatocytes by measuring [3H]S 1743 uptake and in Oatp1-expressing CHO cells by measuring cholyltaurine uptake.