Table 2.
Solubility and microsomal stability of NIQs and their analogues.
| Compound | Solubility |
% Remaining after 30 min |
Microsomal clearance (μl/min/mg) |
||||
|---|---|---|---|---|---|---|---|
| PBS (pH 6.5) | Human | Mouse | Rat | Human | Mouse | Rat | |
| Reserpinea | <5 | – | – | – | – | – | – |
| Hydrocortisonea | 190 | – | – | – | – | – | – |
| Midazolama | – | <7 | <7 | <7 | >250 | >250 | >250 |
| Propranolola | – | 63 | 32 | <7 | 39.6 | 93.9 | >250 |
| MMV390048a | – | 92 | >99 | 97 | <11.6 | <11.6 | <11.6 |
| Dioncophylline C (2a) | 170 | 94 | 95 | 95 | <11.6 | <11.6 | <11.6 |
| Dioncopeltine A (5) | 200 | 98 | <7 | >99 | <11.6 | >250 | <11.6 |
| Atropisomer 2b | 180 | 83 | 32 | 36 | 15.4 | 95.1 | 86.6 |
| Synthetic dimer 9 | 200 | 98 | 99 | 96 | <11.6 | <11.6 | <11.6 |
| Simplified analogue 12 | 180 | 71 | <7 | <7 | 28.2 | >250 | >250 |
a
Reference compounds used in respective assays.