Entecavir monohydrate (BMS-200475) is a selective inhibitor of the replication of the hepatitis B virus (HBV). It, a new deoxyguanine nucleoside analog.

HBV (HepG2 cells):3.75 nM(ec50)

Entecavir在鸭子中,能给与引起血清DHBV DNA水平在80天下降4-log,在血清中乙型肝炎病毒表面抗原在120天内降低 2~ 3-log.Entecavir治疗可以降低肝脏中DHBV DNA复制中间体70倍,而共价闭合环状DNA水平在稳定模板形势下仅降低4倍.在肝脏中,Entecavir治疗降低抗原染色的强度和的抗原-阳性细胞的百分比,但在胆管细胞中抗原染色的强度会出现.

在肝活检标本中,Entecavir能够降低共价闭合环状DNA和乙肝病毒核心抗原阴性。Entecavir三磷酸酯可作为野生型HBV聚合酶的有效抑制剂,是lamivudine三磷酸对3TC耐药HBV聚合酶效果的100～300倍。Entecavir抑制3TC耐药HBV的复制,至少需要达到20~30倍高的浓度。Entecavir在EC 50为0.1 nM时,对HIV具有有效活性。它可以在单周期、单细胞系假病毒测定法测定CD4+淋巴细胞中使用绿色荧光蛋白报告荧光激活细胞分选仪测定。

BMS 200475 is prepared in phosphate-buffered saline (PBS) and diluted with appropriate medium containing 2% fetal bovine serum. HepG2 2.2.15 cells are plated at a density of 5×105 cells per well on 12-well Biocoat collagen-coated plates and are maintained in a confluent state for 2 to 3 days before being overlaid with 1 mL of medium spiked with BMS 200475. Quantification of HBV was performed on day 10[1].