Table 1.
Microsomal stability (MS), hERG inhibition (10 μM), plasma protein binding (PPB), and CYP450 inhibition (10 μM) of cinobufagin (CIN) and telocinobufagin (TEL).
Compound (1 μM) |
MS (% of Remaining) |
hERG Inhibition (%) | PPB (%) | CYP450 Inhibition (%) | |||||||
---|---|---|---|---|---|---|---|---|---|---|---|
Mice | Rat | Human | Mice | Rat | 1A2 | 2C9 | 2C19 | 2D6 | 3A4 | ||
CIN | 0.18 | 4.40 | 2.99 | 24.6 | 90.8 | 78.2 | 4.09 | 33.0 | 46.7 | 11.0 | 6.14 |
±0.07 | ±0.51 | ±0.39 | ±6.82 | ±1.74 | ±8.84 | ±1.0 | ±1.2 | ±9.3 | ±3.9 | ±5.3 | |
TEL | 21.7 | 31.9 | 15.1 | 22.6 | 97.8 | 96.8 | 6.22 | 21.1 | 19.5 | 1.40 | 9.42 |
±0.90 | ±1.31 | ±1.27 | ±6.02 | ±0.35 | ±0.78 | ±1.3 | ±2.8 | ±11.1 | ±3.2 | ±5.3 |