| Description | Doravirine (MK-1439) is a non-nucleoside reverse transcriptase inhibitor, used in the treatment of HIV/AIDS. |
| In vitro | Doravirine 对野生型病毒及K103N、Y181C和K103N/Y181C突变病毒展示出强大的抗病毒活性，其IC50值分别为12、21、31和33 nM。[1] MK-1439 对10种不同HIV-1亚型病毒（共93种病毒）显示出了类似的抗病毒活动。[2] |
| In vivo | 给予高脂餐后服用50 mg doravirine与轻微提升AUC时间零至无限大（AUC0-∞）和C24 h相关，但Cmax没有变化。同时给予doravirine会轻微减少Midazolam的AUC0-∞（几何平均比率0.82，90% CI 0.70, 0.97）。[3] |
| Target activity | K103N/Y181C:33 nM, Virus (WT):12nM, K103N:21nM, Y181C:31nM |
| Synonyms | 多拉维林, 多拉韦林, MK-1439 |
| molecular weight | 425.75 |
| Molecular formula | C17H11ClF3N5O3 |
| CAS | 1338225-97-0 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 45 mg/mL (105.7 mM) |
| References | 1. Lai MT, et al. Antimicrob Agents Chemother. 2014;58(3):1652-63. 2. Anderson MS, et al. Antivir Ther. 2015;20(4):397-405. 3. Fical L. Vývoj UHPLC-MS/MS metody pro analýzu vybraných antivirotik v HILIC a RP módu[J]. 2020 4. Fical L, Khalikova M, Kočová Vlčková H, et al. Determination of Antiviral Drugs and Their Metabolites Using Micro-Solid Phase Extraction and UHPLC-MS/MS in Reversed-Phase and Hydrophilic Interaction Chromatography Modes[J]. Molecules. 2021, 26(8): 2123. |
| Citations | 1. Fical L, Khalikova M, Kočová Vlčková H, et al. Determination of Antiviral Drugs and Their Metabolites Using Micro-Solid Phase Extraction and UHPLC-MS/MS in Reversed-Phase and Hydrophilic Interaction Chromatography Modes. Molecules. 2021, 26(8): 2123. |