| Description | Entecavir (SQ34676) is a guanosine nucleoside analogue used in the treatment of chronic hepatitis B virus (HBV) infection. Entecavir therapy can be associated with flares of the underlying hepatitis B during or after therapy, but has not been linked to cases of clinically apparent liver injury. |
| In vitro | BMS-200475抑制HBV蛋白引物（EC50 值为 3.75 nM），抑制反转录酶的启动。与其他抗RNA和DNA病毒化合物相比，BMS-200475的抗病毒活性显著下降[1]。相对于其他脱氧鸟苷类似物（penciclovir、ganciclovir、lobucavir、aciclovir 或 lamivudine），BMS-200475更容易被磷酸化为其活性代谢物。BMS-200475 的细胞内半衰期为15小时[2]。 |
| In vivo | BMS-200475（p.o ,剂量自0.02至0.5 mg/kg体重，连续1至3个月治疗）能有效降低慢性感染土拨鼠中的土拨鼠乙型肝炎病毒（WHV）血症水平[3]。 |
| Cell experiments | 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]. |
| Target activity | HBV (HepG2 cells):3.75 nM(ec50) |
| Synonyms | BMS200475, SQ34676, 恩替卡韦 |
| molecular weight | 277.28 |
| Molecular formula | C12H15N5O3 |
| CAS | 142217-69-4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 55 mg/mL (198.36 mM) |
| References | 1. Sham, H., Kempf, D., Molla, A., Marsh, K., Kumar, G., & Chen, C. et al. (1998). ABT-378, a Highly Potent Inhibitor of the Human Immunodeficiency Virus Protease. Antimicrobial Agents And Chemotherapy, 42(12), 3218-3224. doi: 10.1128/aac.42.12.3218 2. Xie B, Sun D, Du Y, et al. A two-step lineage reprogramming strategy to generate functionally competent human hepatocytes from fibroblasts[J]. Cell research. 2019: 1. |
| Citations | 1. Xie B, Sun D, Du Y, et al. A two-step lineage reprogramming strategy to generate functionally competent human hepatocytes from fibroblasts. Cell research. 2019: 1. 2. Yang Y, Yan Y, Yin J, et al. Structure-Based Discovery of N-Sulfonylpiperidine-3-carboxamides as Novel Capsid Assembly Modulators for Potent Inhibition of HBV Replication. Viruses. 2022, 14(2): 348. 3. Yin J, Feng Z, Li Z, et al.Synthesis and evaluation of N-sulfonylpiperidine-3-carboxamide derivatives as capsid assembly modulators inhibiting HBV in vitro and in HBV-transgenic mice.European Journal of Medicinal Chemistry.2023: 115141. 4. Bao H, Yan J, Huang J, et al.Activation of endogenous retrovirus triggers microglial immuno-inflammation and contributes to negative emotional behaviors in mice with chronic stress.Journal of Neuroinflammation.2023, 20(1): 1-16. 5. Yang L, Gong Y, Liu F, et al.A novel phthalazinone derivative as a capsid assembly modulator inhibits hepatitis B virus expression.Antiviral Research.2023: 105763. |