MK-0608

产品编号 T16088Cas号 443642-29-3

MK-0608 是一种可口服的体外 HCV 复制抑制剂。在亚基因组复制子测定中，EC50值为 0.3 μM，EC90值为 1.3 μM。

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产品编号 T16088Cas号 443642-29-3

MK-0608 是一种可口服的体外 HCV 复制抑制剂。在亚基因组复制子测定中，EC50值为 0.3 μM，EC90值为 1.3 μM。

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生物活性

产品描述	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).
靶点活性	HCV replication:(EC50)0.3 μM
体内活性	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。
动物实验	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.

化学信息

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

溶解度信息

DMSO: 27.5 mg/mL (98.12 mM)

溶液配制表

DMSO