Adefovir
(Synonyms: 阿德福韦; GS-0393; PMEA) 目录号 : GC42731An active metabolite of adefovir dipivoxil
Cas No.:106941-25-7
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.00%
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Animal experiment |
Animal Models: Ducks |
Adefovir is an acyclic nucleoside phosphonate that acts as a reverse transcriptase inhibitor. When evaluated in animal and clinical models of infections, its antiviral spectrum was shown to uniquely encompass activity against herpes viruses (HSV-1, HSV-2, VZV, CMV, EBV, HHV-6, HHV-7, and HHV-8), hepatitis B virus (HBV), and HIV (HIV-1, HIV-2, SIV, and FIV). Adefovir-associated resistance mutations have not yet been observed in HBV resistance surveillance clinical studies.
Cas No. | 106941-25-7 | SDF | |
别名 | 阿德福韦; GS-0393; PMEA | ||
Canonical SMILES | NC1=C2C(N(CCOCP(O)(O)=O)C=N2)=NC=N1 | ||
分子式 | C8H12N5O4P | 分子量 | 273.2 |
溶解度 | 0.1 M NaOH : 10 mg/mL (36.60 mM; ultrasonic and adjust pH to 10 with NaOH) | 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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 3.6603 mL | 18.3016 mL | 36.6032 mL |
5 mM | 0.7321 mL | 3.6603 mL | 7.3206 mL |
10 mM | 0.366 mL | 1.8302 mL | 3.6603 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 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Adefovir for lamivudine-resistant hepatitis B
Antivir Ther 2022 Apr;27(2):13596535211067605.PMID:35499182DOI:10.1177/13596535211067605.
Adefovir, a nucleotide analog developed by John Martin, was a major breakthrough in the treatment of chronic Hepatitis B. Prior to Adefovir, Hepatitis B treatment was limited to two therapeutic modalities, either interferon, which carried significant side effects and was efficacious in a minority of patients, or lamivudine which showed no durable effects with short-term use and a high rate of resistance with long-term use. Adefovir was found to be effective in suppressing viral replication and in resolving the hepatic inflammation associated with hepatitis B with only rare instances of resistance. In this article, we appreciate John Martin's contribution to science and medicine as we review the landmark trials of Adefovir that brought forth a new era of treatment of Hepatitis B.
Adefovir dipivoxil in the treatment of chronic hepatitis B virus infection
Expert Rev Anti Infect Ther 2004 Aug;2(4):475-83.PMID:15482214DOI:10.1586/14787210.2.4.475.
Adefovir dipivoxil (Hepsera, Gilead Sciences) is a prodrug of Adefovir, with potent antiviral activity against hepatitis B virus. Adefovir dipivoxil therapy, 10 mg daily for 48 weeks, is effective in hepatitis B e antigen-positive and -negative chronic hepatitis B. In hepatitis B e antigen-negative chronic hepatitis B, Adefovir dipivoxil was recently found to maintain its efficacy even after 3 years of therapy. Adefovir dipivoxil is effective in patients with compensated or decompensated chronic viral B liver disease, and in pre- and post-transplant hepatitis B virus patients who develop resistance to lamivudine (Epivir, GlaxoSmithKline). It is well-tolerated and safe even after the third year of long-term therapy, and is associated with low rates of viral resistance. All these characteristics make Adefovir dipivoxil an important drug for the treatment of hepatitis B virus infection and an excellent candidate for long-term maintenance therapy in chronic viral B liver disease.
Evaluation of Ion-pair Formation of Adefovir to Improve Permeation across Artificial and Biological Membranes
J Pharm Pharm Sci 2018;21(1):160-170.PMID:29789103DOI:10.18433/jpps29394.
Purpose: Adefovir is an antiviral drug that exhibits high hydrophilic properties and negligible bioavailability (less than 12%). It is only applied in the form of the ester prodrug Adefovir dipivoxil (ADV). The oral bioavailability of ADV is limited (32% to 45%) by its low permeability (Class 3) and biological conversion of the prodrug to Adefovir. Ion-pair formation is considered as an alternative approach to a covalent prodrug (ADV) to enhance intestinal permeation of Adefovir. Methods: The effect of various counter-ions (anionic, cationic and two quaternary ammonium salts) on the lipophilicity of Adefovir was investigated by means of the n-octanol/buffer partitioning system, an in vitro transport model (PAMPA) and a biological membrane (everted gut sac). Results: Quaternary ammonium salts, cetylpyridinium chloride (CPC) and cetrimide enhanced the lipophilicity of Adefovir 136- and 87-fold, respectively. The apparent permeability of Adefovir in combination with CPC (counter-ion) was 2.5-fold greater than ADV permeability in the PAMPA model. The apparent permeability of adefovir-CPC (counter-ion) was 1.3-fold greater than that of Adefovir dipivoxil permeability in a biologic membrane (everted gut sac). Conclusion: These results suggest that the adefovir-CPC ion-paired system has potential for improving the permeation of Adefovir across the intestinal membrane. This article is open to POST-PUBLICATION REVIEW. Registered readers (see "For Readers") may comment by clicking on ABSTRACT on the issue's contents page.
Comparison of the efficacy of tenofovir and Adefovir in the treatment of chronic hepatitis B: a systematic review
Virol J 2011 Mar 9;8:111.PMID:21388525DOI:10.1186/1743-422X-8-111.
Chronic viral hepatitis B remains a global public health concern. Currently, several drugs, such as tenofovir and Adefovir, are recommended for treatment of patients with chronic hepatitis B. tenofovir is a nucleoside analog with selective activity against hepatitis b virus and has been shown to be more potent in vitro than Adefovir. But the results of trials comparing tenofovir and Adefovir in the treatment of chronic hepatitis B were inconsistent. However, there was no systematic review on the comparison of the efficacy of tenofovir and Adefovir in the treatment of chronic hepatitis B. To evaluate the comparison of the efficacy of tenofovir and Adefovir in the treatment of chronic hepatitis B we conducted a systematic review and meta-analysis of clinical trials. We searched PUBMED, Web of Science, EMBASE, CNKI, VIP database, WANFANG database, the Cochrane Central Register of Controlled Trials and the Cochrane Database of Systematic Review. Finally six studies were left for analysis which involved 910 patients in total, of whom 576 were included in tenofovir groups and 334 were included in Adefovir groups. At the end of 48-week treatment, tenofovir was superior to Adefovir at the HBV-DNA suppression in patients[RR = 2.59; 95%CI(1.01-6.67), P = 0.05]. While there was no significant difference in the ALT normalization[RR = 1.15; 95%CI(0.96-1.37), P = 0.14], HBeAg seroconversion[RR = 1.32; 95%CI(1.00-1.75), P = 0.05] and HBsAg loss rate[RR = 1.19; 95%CI(0.74-1.91), P = 0.48]. More high-quality, well-designed, randomized controlled, multi-center trails are clearly needed to guide evolving standards of care for chronic hepatitis B.
Comparison of the efficacy of Lamivudine plus Adefovir versus entecavir in the treatment of Lamivudine-resistant chronic hepatitis B: a systematic review and meta-analysis
Clin Ther 2013 Dec;35(12):1997-2006.PMID:24238791DOI:10.1016/j.clinthera.2013.10.002.
Background: Hepatitis B virus infection remains 1 of the major health threats worldwide. Currently, lamivudine plus Adefovir combination therapy or entecavir monotherapy is usually used for the treatment of patients with lamivudine-resistant chronic hepatitis B (CHB). However, there are few systematic comparisons between the efficacy of lamivudine plus Adefovir and the efficacy of entecavir in the treatment of these patients. Objective: The goal of this systematic study and meta-analysis was to assess the efficacy of lamivudine plus Adefovir compared with entecavir for the treatment of patients with lamivudine-resistant CHB. Methods: A comprehensive literature search of PUBMED, Web of Science, WANFANG database, the Cochrane Central Register of Controlled Trials, and the Cochrane Database of Systematic Review, were screened to obtain citations from January 1990 to January 2012 in this study. Data analysis was done by using the Review Manager Software 5.1. Results: Eight studies were suitable for analysis. A total of 696 patients with lamivudine-resistant CHB were studied and grouped according to treatment: 341 patients in the entecavir group and 355 patients in the lamivudine plus Adefovir group. The results found that the rates of undetectable hepatitis B virus DNA levels, alanine aminotransferase normalization, hepatitis B e antigen loss, and hepatitis B e antigen seroconversion were not significantly different between the lamivudine plus Adefovir group and the entecavir group. Moreover, the rate of adverse reactions was also not significantly different between the 2 groups. However, virologic breakthrough for the patients with lamivudine resistance was higher in the entecavir group than in the lamivudine plus Adefovir group. Conclusions: For these CHB patients with lamivudine resistance, lamivudine plus Adefovir was a better treatment option than entecavir alone.