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. 2021 Nov 2;13(11):1839. doi: 10.3390/pharmaceutics13111839

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