| Description | Lagociclovir (MIV-210), a nucleoside analogue, is an antiviral compound available for the treatment of HBV82 that inhibits the replication of wild-type hepatitis B virus (HBV) in human hepatocellular carcinoma cell lines that permanently express HBV. |
| In vitro | Lagociclovir（FLG）（6天）在暂时转染的Huh7细胞中对3TC-R HBV、wt HBV、PMEA-R HBV及3TC+PMEA-R HBV表现出抑制活性，其IC50分别为8 ± 3.8、9 ± 2.5、13 ± 3.4及15 ± 6.8μM[1]。Lagociclovir（0-100 μM；6天）能够抑制在暂时转染的Huh7细胞中HBV野生型及耐药变异体的复制[2]。 |
| In vivo | 口服抗-HBV化合物Lagociclovir（20或60mg/kg；体重/天）在慢性感染的土拨鼠模型中快速引发了抗病毒反应，2周内分别使血清WHV DNA水平降低4.75 log10和5.72 log10。Lagociclovir以20或60mg/kg/天的剂量，将肝脏WHV DNA负荷从治疗前水平降低200至2500倍。此外，每日剂量10mg/kg在治疗4周后使血清WHV负荷降低400倍，并且5mg/kg/天的剂量足以在接下来的6周期间维持这种抗病毒效果。[1] |
| Target activity | HBV (3TC+PMEA-R):15 μM, HBV (WT):9 μM, PMEA-R (HBV):13 μM, HBV (3TC-R):8 μM |
| Synonyms | MIV-210 |
| molecular weight | 269.23 |
| Molecular formula | C10H12FN5O3 |
| CAS | 92562-88-4 |
| Storage | |Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 25 mg/mL (92.86 mM) |
| References | 1. Michalak TI, et al. Profound antiviral effect of oral administration of MIV-210 on chronic hepadnaviral infection in a woodchuck model of hepatitis B. Antimicrob Agents Chemother. 2009;53(9):3803-3814. 2. Jacquard AC, et al. In vitro characterization of the anti-hepatitis B virus activity and cross-resistance profile of 2',3'-dideoxy-3'-fluoroguanosine. Antimicrob Agents Chemother. 2006;50(3):955-961. 3. De Clercq E. Emerging anti-HIV drugs. Expert Opin Emerg Drugs. 2005;10(2):241-273. |