| Description | Adefovir dipivoxil (GS 0840) is a dipivoxil formulation of adefovir, a nucleoside reverse transcriptase inhibitor analog of adenosine with activity against hepatitis B virus (HBV), herpes virus, and human immunodeficiency virus (HIV). |
| In vitro | 相比安慰剂对照组的5.3 log10的GE/毫升,Adefovir Dipivoxil减少转基因小鼠血清HBV DNA至3.5 log10的基因组等同物/ mL的表达乙型肝炎病毒.Adefovir Dipivoxil在肝脏中,抗病毒活性在第10天达到最大值,在1.0 mg/kg/天到达的乙肝病毒抑制的端点.Adefovir Dipivoxil降低肝脏HBV DNA至<0.1皮克乙肝病毒每转基因小鼠的总DNA（皮克/毫克）. |
| In vivo | 在鸭的HBV（DHBV）模型中,Adefovir dipivoxil和其他核苷类似物（拉米夫定,恩替卡韦,恩曲他滨 [FTC]和替比夫定 [L-dT]）联用产生比单独用药更好的抗病毒效果。同一模型中,Adefovir dipivoxil能够在体外和体内抑制病毒CCC DNA。当Adefovir加入细胞很短时间就能保留明显的抗HBV活性。Adefovir和拉米夫定,FTC,或L-dT联用时具有累积效应和恩替卡韦或替诺福韦联用时表现协同效应。Adefovir dipivoxil的前基因组RNA的转录后抑制聚合酶的活性。 Adefovir dipivoxil剂量依赖性地抑制培养上清液中病毒的释放和细胞内病毒DNA的合成。 |
| Synonyms | Hepsera, GS 0840, 阿德福韦酯, Preveon |
| molecular weight | 501.47 |
| Molecular formula | C20H32N5O8P |
| CAS | 142340-99-6 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | H2O: < 1 mg/mL (insoluble or slightly soluble) DMSO: 93 mg/mL (185.5 mM) Ethanol: 93 mg/mL (185.5 mM) |
| References | 1. Julander JG, et al. Antiviral Res, 2002, 55(1), 27-40. 2. Delmas J, et al. Antimicrob Agents Chemother, 2002, 46(2), 425-433. 3. Delaney WE 4th, et al. Antimicrob Agents Chemother, 2004, 48(10), 3702-3710. 4. Ying, et al. J Viral Hepat, 2000, 7(1), 79-83. 5. Chen X, et al. J Natl Cancer Inst, 2003, 95(14), 1053-1061. 6. Thieulent C, Hue E, Sutton G, et al. Identification of antiviral compounds against equid herpesvirus-1 using real-time cell assay screening: efficacy of decitabine and valganciclovir alone or in combination[J]. Antiviral Research. 2020: 104931 |
| Citations | 1. Thieulent C, Hue E, Sutton G, et al. Identification of antiviral compounds against equid herpesvirus-1 using real-time cell assay screening: efficacy of decitabine and valganciclovir alone or in combination. Antiviral Research. 2020: 104931 2. Dsouza L, Pant A, Offei S, et al.Antiviral activities of two nucleos (t) ide analogs against vaccinia, mpox, and cowpox viruses in primary human fibroblasts.Antiviral Research.2023: 105651. |