Table 3. DGAT1 Activities and Solubility of Racemates 12a and 12g and Their Corresponding Enantiomers (S-12a, R-12a, and S-12g, R-12g).
compd # | hDGAT1 CPM IC50 (nM)a | hDGAT1 LE IC50 (nM)a | rDGAT1 LE IC50 (nM)a | C2C12 Inh. at 300 nM (%)a | solubility (μg/mL)a |
---|---|---|---|---|---|
12a (Rac) | 3 | 8 | 158 | 62 | 39 |
S-12a | 2.5 | 1 | 126 | 75 | 78 |
R-12a | 126 | 251 | 631 | 27 | 88 |
12g (Rac) | 2 | NDb | NDb | 72 | 100 |
S-12g | 2 | 8 | 158 | 83 | 5 |
R-12g | 158 | NDb | 1260 | NDb | 0.4 |
Value is an average of at least n = 2.
ND = not determined.