Adefovir Dipivoxil是一种口服有效的逆转录酶抑制剂。
Cas No.:142340-99-6
Sample solution is provided at 25 µL, 10mM.
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Adefovir Dipivoxil is an orally effective reverse transcriptase inhibitor. Adefovir Dipivoxil is a prodrug form of adefovir, and compared to free adefovir, it has higher oral bioavailability in dogs, mice, rats, and monkeys. Adefovir Dipivoxil acts as a chain terminator nucleotide analog and is effective against some retroviruses, herpesviruses, and hepadnaviruses including HBV[1][2][3].
In vitro, Adefovir Dipivoxil at 0.03-30µM dose-dependently inhibited the proliferation of H1975, A549 and PC9 cells after 6 days of treatment, with IC₅₀ values of 2.68, 11.84 and 1.77µM, respectively[2]. Adefovir Dipivoxil at 1µM for 3 days enhanced 1,25(OH)₂D₃-induced basolateral-to-apical transport and increased the efflux ratio in Caco-2 cells[4].
In vivo, oral administration of Adefovir Dipivoxil at 100mg/kg twice daily for 10 days reduced hepatic HBV DNA to 0.1pg/g total DNA and serum HBV DNA to 3.5 log₁₀ ge/mL in HBV transgenic mice, compared with 3.0pg/g and 5.3 log₁₀ ge/mL in controls; with once-daily dosing, antiviral activity approached maximal liver viral reduction by day 10, reaching an endpoint at 1.0mg/kg/d, while the minimum effective dose based on serum virus inhibition was below 0.1mg/kg/day[3]. Adefovir Dipivoxil administered intraperitoneally at 5mg/kg once daily for 5 days effectively protected mice from lethal pseudorabies virus (PRV) infection[5].
References:
[1] Annaert P, Tukker JJ, van Gelder J, et al. In vitro, ex vivo, and in situ intestinal absorption characteristics of the antiviral ester prodrug adefovir dipivoxil. J Pharm Sci. 2000;89(8):1054-1062.
[2] Patel A, Seraia E, Ebner D, Ryan AJ. Adefovir dipivoxil induces DNA replication stress and augments ATR inhibitor-related cytotoxicity. Int J Cancer. 2020;147(5):1474-1484.
[3] Julander JG, Sidwell RW, Morrey JD. Characterizing antiviral activity of adefovir dipivoxil in transgenic mice expressing hepatitis B virus. Antiviral Res. 2002;55(1):27-40.
[4] Maeng HJ, Chapy H, Zaman S, Pang KS. Effects of 1α,25-dihydroxyvitamin D3 on transport and metabolism of adefovir dipivoxil and its metabolites in Caco-2 cells. Eur J Pharm Sci. 2012;46(3):149-166.
[5] Wang G, Chen R, Huang P, et al. Adefovir dipivoxil efficiently inhibits the proliferation of pseudorabies virus in vitro and in vivo. Antiviral Res. 2021;186:105014.
Adefovir Dipivoxil是一种口服有效的逆转录酶抑制剂。Adefovir Dipivoxil是adefovir的前药形式，与游离adefovir相比，它在狗、小鼠、大鼠和猴子中具有更高的口服生物利用度。Adefovir Dipivoxil作为一种链终止核苷酸类似物，对一些逆转录病毒、疱疹病毒和肝病毒（包括HBV）有效[1][2][3]。
体外实验中，Adefovir Dipivoxil在0.03–30µM范围内处理6天，可剂量依赖性抑制H1975，A549和PC9细胞的增殖，其IC₅₀值分别为2.68，11.84和1.77µM[2]。Adefovir Dipivoxil以1µM处理3天，可增强1,25(OH)₂D₃诱导的Caco-2细胞中基底侧向顶端的转运，并提高外排比[4]。
体内实验中，在HBV转基因小鼠中，口服给予Adefovir Dipivoxil（100mg/kg，每日两次）连续10天后，肝脏HBV DNA降至0.1pg/g总DNA，血清HBV DNA降至3.5 log₁₀ ge/mL，而对照组分别为3.0pg/g和5.3 log₁₀ ge/mL；在每日一次给药条件下，其抗病毒活性在第10天接近肝脏病毒降低的最大水平，并在1.0mg/kg/天达到抑制终点，而基于血清病毒抑制的最小有效剂量低于0.1mg/kg/天[3]。Adefovir Dipivoxil以5mg/kg的剂量腹腔注射，每天1次，连续5天，可有效保护小鼠免受致命性伪狂犬病毒（PRV）感染[5]。
| Cell experiment [1]: | |
Cell lines | H1975, A549 and PC9 |
Preparation Method | H1975, A549, PC9 cell lines were treated with 0.03-30µM Adefovir Dipivoxil for 6 days. On day 6 a resazurin proliferation assay was performed. |
Reaction Conditions | 0.03-30µM; 6d |
Applications | Adefovir Dipivoxil at 0.03-30µM dose-dependently inhibited the proliferation of H1975, A549, and PC9 cells after 6 days of treatment, with IC₅₀ values of 2.68, 11.84 and 1.77µM, respectively. |
| Animal experiment [2]: | |
Animal models | Male HBV transgenic mice |
Preparation Method | Male transgenic mice were divided into groups of five animals and treated twice daily (bid) with oral Adefovir Dipivoxil (ADV) at 100mg/kg/day for 10 days. A saline-treated group and an untreated group were used as controls for this experiment. Tissue samples were obtained on the last day of the experiment 2-4h after the last treatment. |
Dosage form | 100mg/kg; bid for 10 days; p.o. |
Applications | Oral ADV administered twice daily reduced the liver HBV DNA to near the levels of detection (0.02pg viral DNA/μg cellular DNA) as compared to the saline control values (3.0pg/μg) Viral signals of the Southern blot from mice treated with ADV were generally a lower intensity ADV had no significant effect on core antigen (HBcAg) in the liver or pre-core antigen (HBeAg) in the serum. |
References: | |
| Cas No. | 142340-99-6 | SDF | |
| 别名 | 阿德福韦酯; GS 0840 | ||
| 化学名 | [2-(6-aminopurin-9-yl)ethoxymethyl-(2,2-dimethylpropanoyloxymethoxy)phosphoryl]oxymethyl 2,2-dimethylpropanoate | ||
| Canonical SMILES | CC(C)(C)C(=O)OCOP(=O)(COCCN1C=NC2=C1N=CN=C2N)OCOC(=O)C(C)(C)C | ||
| 分子式 | C20H32N5O8P | 分子量 | 501.47 |
| 溶解度 | ≥ 18.7mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9941 mL | 9.9707 mL | 19.9414 mL |
| 5 mM | 398.8 μL | 1.9941 mL | 3.9883 mL |
| 10 mM | 199.4 μL | 997.1 μL | 1.9941 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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