| Bioactivity | 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)[1]. |
| In Vivo | hCYP3A4-IN-1 (compound C6) 在 HLM 中表现出适当的代谢稳定性，并在小鼠中表现出良好的安全性[1]。hCYP3A4-IN-1 (100 mg/kg，口服给药，一次)显著增加 midazolam（灌胃，10 mg/kg）的 AUC(0-inf) 3.63 倍，并强烈延长其小鼠体内的半衰期，是溶剂组的 1.66 倍[1]。Pharmacokinetic Parameters of hCYP3A4-IN-1 in mice[1]. |
| Name | hCYP3A4-IN-1 |
| Formula | C20H18N2O |
| Molar Mass | 302.37 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Lu S, et al. Design, synthesis and biological evaluation of chalcone derivatives as potent and orally active hCYP3A4 inhibitors. Bioorg Med Chem Lett. 2023 Aug 5:129435. |