hCYP3A4-IN-1
hCYP3A4-IN-1 (compound C6) is a potent, orally active hCYP3A4 inhibitor. hCYP3A4-IN-1 shows the IC50 values of 43.93 nM and 153.00 nM against hCYP3A4 in human liver microsomes (HLMs) and CHO-3A4 stably transfected cell line, respectively. hCYP3A4-IN-1 potently inhibits CYP3A4-catalyzed N-ethyl-1,8-naphthalimide (NEN) hydroxylation in a competitive manner (Ki = 30.00 nM).
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- CAS 番号: 3003751-14-9
- 分子式: C20H18N2O
- 分子量:302.37
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生物活性
製品説明
IC50 & Target
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CYP3A4 43.93 nM (IC50) |
体内実験
hCYP3A4-IN-1 (100 mg/kg, orally administration, once) significantly increases the AUC(0-inf) of midazolam (i.g. 10 mg/kg) by 3.63-fold, and strongly prolonged its half-life by 1.66-fold compared with the vehicle group in mice[1].
Pharmacokinetic Parameters of hCYP3A4-IN-1 in mice[1].
| CMC-Na + Midazolam | C6 (25 mg/kg) + Midazolam | C6 (100 mg/kg) + Midazolam | |
| Tmax (min) | 8.00 ± 2.74 | 5.83 ± 2.04 | 10.00 ± 0.00 |
| Cmax (ng/mL) | 194.20 ± 138.88 | 312.00 ± 141.40 | 494.67 ± 210.22 |
| AUC0-24 (ng/mL∗min) | 7520.83 ± 2413.78 | 14784.92 ± 3501.33 | 27330.95 ± 6664.85 |
| t1/2 (min) | 36.33 ± 14.46 | 54.96 ± 20.87 | 60.37 ± 27.67 |