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Adefovir

CAS No. : 106941-25-7

MCE 站：Adefovir

产品活性：Adefovir (GS-0393) 是一种单磷酸腺苷类似物抗病毒剂，在细胞内转化为 Adefovir diphosphate 后可抑制 HBV DNA 聚合酶。Adefovir 在 HepG2.2.15 细胞系中对 HBV 的 IC₅₀ 为 0.7 μM。Adefovir 对多种病毒(包括 HBV 和疱疹病毒)具有良好的抗病毒活性。

研究领域：Anti-infection

作用靶点：HBV  |  Reverse Transcriptase

In Vitro: Studies to elucidate the mechanism of action of Adefovir against herpesvirus replication reveals that the phosphorylation of Adefovir occurred intracellularly and is carried out by host cellular enzymes. The diphosphorylated derivatives of Adefovir targeted the viral DNA polymerase and also acted as DNA chain terminators. Adenylate kinase is shown to be responsible for the first phosphorylation, which was followed by ADP kinase and creatine kinase, forming Adefovir diphosphate.

In Vivo: Unaffected by food, Adefovir achieves 60% oral bioavailability. Its half-life is 12-30 hours and Adefovir undergoes renal excretion without significant metabolites. Adefovir does not substantially affect the cytochrome P450 system.

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