| Description | MK-0608 is an orally bioavailable HCV replication inhibitor in vitro(EC50 = 0.3 μM and EC90=1.3 μM in the subgenomic-replicon assay). |
| In vivo | MK-0608在1b型HCV亚基因组复制子中抑制病毒RNA的复制，其50%有效浓度（EC(50)）为0.3微摩尔（EC(90) = 1.3微摩尔）。MK-0608对HCV感染的黑猩猩进行治疗时显示出强大的抗病毒效果。 |
| Animal experiments | MK-0608 was administered to HCV-infected chimpanzees, resulting in dose- and time-dependent decreases in plasma viral loads.?In separate experiments, chimpanzees dosed for 7 days with MK-0608 at 0.2 and 2 mg per kg of body weight per day by intravenous administration experienced average reductions in viral load of 1.0 and >5 log(10) IU/ml, respectively.?Two other HCV-infected chimpanzees received daily doses of 1 mg MK-0608 per kg via oral administration.?After 37 days of oral dosing, one chimpanzee with a high starting viral load experienced a reduction in viral load of 4.6 log(10), and the viral load in the other chimpanzee fell below the limit of quantification (LOQ) of the HCV TaqMan assay (20 IU/ml).?Importantly, viral load remained below the LOQ throughout the duration of dosing and for at least 12 days after dosing ended. |
| Target activity | HCV replication:(EC50)0.3 μM |
| molecular weight | 280.28 |
| Molecular formula | C12H16N4O4 |
| CAS | 443642-29-3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 27.5 mg/mL (98.12 mM) |
| References | 1. Carroll SS, et al. Robust antiviral efficacy upon administration of a nucleoside analog to hepatitis C virus-infected chimpanzees. Antimicrob Agents Chemother. 2009 Mar;53(3):926-34. |