Table 3. Pharmacokinetic Properties and Cellular Activity of Compound 19a.
IC50 [μM] | PKC-ι | 0.34 |
GI50 [μM] | Huh-7 | 11.3 |
in vitro PK | Sol (pH 7.4, μg/mL) | 164 |
Caco-2 (A–B, 10–6 cm/s) | 0.28 | |
MLM/HLM (CL, μL/min/mg) | 71/5.1 |
PKC-ι inhibitor CRT006685412 was used as a positive control; GI50 against HUH-7 cells was 3.1 μM.