Effector | Parameter | rCYP3A4 | rCYP3A5 | HLMs | Human Hepatocytes |
---|---|---|---|---|---|
Androstenedione | Heteroactivation ratio | 4.9 | 7.6 | 18.5 | 7.3 |
Unbound EC200 (μM) | 2.5 | — | 0.9 | 0.5 | |
fuinc | — | — | 0.54 | 0.70 | |
Testosterone | Heteroactivation ratio | 4.0 | 11.9 | 8.8 | 6.1 |
Unbound EC200 (μM) | 3.2 | — | 0.8 | 1.2 | |
fuinc | — | — | 0.54 | 0.62 | |
Progesterone | Heteroactivation ratio | 4.7 | 10.8 | 6.7 | 4.3 |
Unbound EC200 (μM) | 3.1 | — | 0.5 | 2.2 | |
fuinc | — | — | 0.17 | 0.43 | |
Aldosterone | Heteroactivation ratio | 6.3 | 8.4 | 10.5 | 5.5 |
Unbound EC200 (μM) | 24.1 | — | 7.1 | 31.5 | |
fuinc | — | — | 0.65 | 0.70 | |
α-Naphthoflavone | Heteroactivation ratio | 2.5 | — | 2.9 | 3.7 |
Unbound EC200 (μM) | 1.2 | — | 0.2 | 0.1 | |
fuinc | — | — | 0.02 | 0.05 | |
Flavone | Heteroactivation ratio | 5.8 | 3.8 | 7.2 | 19.5 |
Unbound EC200 (μM) | 5.9 | — | 1.8 | 0.7 | |
fuinc | — | — | 0.15 | 0.15 | |
DHEA | Heteroactivation ratio | 6.0 | 15.7 | 14.1 | 11.0 |
Unbound EC200 (μM) | 2.2 | — | 1.2 | 0.8 | |
fuinc | — | — | 0.49 | 0.49 | |
DHEA-S | Heteroactivation ratio | — | 3.6 | — | 2.6 |
Unbound EC200 (μM) | — | — | — | 9.3 | |
fuinc | — | — | 0.33 | 0.33 | |
Cortisol | Heteroactivation ratio | 2.3 | 2.4 | 2.4 | 3.6 |
Unbound EC200 (μM) | 46.0 | — | 14.4 | 5.5 | |
fuinc | — | — | 0.25 | 0.35 | |
Quinidine | Heteroactivation ratio | — | — | — | — |
Unbound EC200 (μM) | — | — | — | — | |
| fuinc | — | — | 0.45 | 0.72 |
—, not determined