Table 3. In Vitro and in Vivo Inhibition of de Novo Palmitate Synthesis by Compound 19.
human IC50 (HeLa, μM) | rat IC50 (NMU, μM) |
---|---|
in vitro | |
0.012 | 0.062 |
rat no. | [19]liverb (μM) | % inhibitionc |
---|---|---|
in vivo: 15 mg/kga | ||
1 | 1.7 | 33 |
2 | 0.16 | 2 |
3 | 0.13 | 9 |
4 | 2.9 | 35 |
5 | 8.1 | 70 |
in vivo: 50 mg/kga | ||
1 | 23.6 | 91 |
2 | 14.4 | 96 |
3 | 12.6 | 52 |
4 | 9.8 | 100 |
5 | 3.4 | 40 |
Oral dose.
Liver level of 19 at 8 h.
% inhibition of de novo palmitate synthesis at 8 h as compared to vehicle group.