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Adefovir

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Chemical Structure| 106941-25-7 同义名 : GS-0393;PMEA
CAS号 : 106941-25-7
货号 : A176069
分子式 : C8H12N5O4P
纯度 : 99%
分子量 : 273.186
MDL号 : MFCD00866943
存储条件：

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

H2O: 1 mg/mL(3.66 mM)，配合低频超声，并水浴加热至45℃助溶

0.1 M NaOH: 10 mg/mL(36.61 mM)，配合低频超声，并调节pH至10
动物实验配方：
生物活性
描述 The herpesviruses comprise a large family of viruses infecting most vertebrates. The virus particle is about 100 nm in diameter and consists of an icosahedral nucleocapsid surrounded by an outer membrane. A critical defining property of the herpesviruses is their ability to form a latent infection as part of their life cycle. Adefovir has been shown to have good antiviral activity against several viruses, including HIV and HBV, and herpesviruses, such as HSV (herpes simplex virus), EBV (Epstein–Barr virus), VZV (varicella zoster virus), and CMV (cytomegalovirus). Adefovir has an IC50 of 0.7 μM against HBV in the HepG2.2.15 cell line[3]. The effect of adefovir on viral CCC DNA (covalently closed circular DNA) synthesis was examined with primary cultures of DHBV (duck HBV)-infected fetal hepatocytes. Adefovir was administered for six consecutive days starting one day before or four days after DHBV inoculation. Dose-dependent inhibition of both virion release in culture supernatants and synthesis of intracellular viral DNA was observed. Preventive treatment of experimentally infected ducklings with adefovir revealed that it efficiently suppressed viremia and intrahepatic DNA[4]. The steady-state volume of distribution of adefovir in patients was found to be about 0.4 L/kg[3].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00798460 Chronic Hepatitis B Phase 4 Terminated(could not enroll pa... 展开 >>tients) 收起 << - Korea, Republic of ... 展开 >> Ilsanpaik hospital Goyang, Gyunggi, Korea, Republic of, 411-706 收起 <<
NCT02826070 Hepatitis B, Chronic Phase 4 Unknown October 2017 China, Beijing ... 展开 >> 302 Military Hospital Of China Beijing, Beijing, China Beijing Ditan Hospital Beijing, Beijing, China BeiJing YouAn Hospital ,Capital Medical University Beijing, Beijing, China Department of infectious disease, First Hospital of Peking University Beijing, Beijing, China People's Hospital of Beijing University Beijing, Beijing, China China, Chongqing The Second Affiliated of ChongQing University of Medical Science Chongqing, Chongqing, China China, Guangdong Department of Infectious Disease, Nanfang Hospital Guangzhou, Guangdong, China No. 8 People's Hospital In GuangZhou Guangzhou, Guangdong, China The Third Hospital of Sun Yat-Sen University Guangzhou, Guangdong, China China, Hubei Tongji Hospital of Tongji Medical College of Huazhong University of Science and Technology Wuhan, Hubei, China China, Hunan Xiangya Hospital Central-South Univrsity Changsha, Hunan, China China, Jiangsu No.81 Hospital of PLA Nanjing, Jiangsu, China China, Jilin First Hospital .Jilin Unniversity Changchun, Jilin, China China, Liaoning ShengJing Hospital of China Medical University Shengyang, Liaoning, China China, Shandong JiNan Infectious Diseases Hospital Jinan, Shandong, China China, Shanghai Changhai Hospital affiliated to Second Military Medical University Shanghai, Shanghai, China Huashan Hospital，Fudan University Shanghai, Shanghai, China Shanghai Ruijin Hospital Shanghai, Shanghai, China China, Shanxi Tangdu Hospital XiAn, Shanxi, China China, Zhejiang The First Affiliated Hospital of College of Medicine, Zhejiang University Hangzhou, Zhejiang, China 收起 <<
NCT00199732 - Completed - France ... 展开 >> Service d'Hépato-gastroentérologie Limoges, France Service de Médecine Interne Limoges, France Service de Virologie Limoges, France Service des Maladies Infectieuses et Tropicales Limoges, France 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.66mL

0.73mL

0.37mL

18.30mL

3.66mL

1.83mL

36.61mL

7.32mL

3.66mL
参考文献

[1]Hachiya A, Kodama EN, et al. K70Q adds high-level tenofovir resistance to "Q151M complex" HIV reverse transcriptase through the enhanced discrimination mechanism. PLoS One. 2011 Jan 13;6(1):e16242.

[2]Perno CF, Yarchoan R, et al. Different pattern of activity of inhibitors of the human immunodeficiency virus in lymphocytes and monocyte/macrophages. Antiviral Res. 1992 Apr;17(4):289-304.

[3]7.11 - Deoxyribonucleic Acid Viruses: Antivirals for Herpesviruses and Hepatitis B Virus

[4]Delmas J, Schorr O, Jamard C, et al. Inhibitory effect of adefovir on viral DNA synthesis and covalently closed circular DNA formation in duck hepatitis B virus-infected hepatocytes in vivo and in vitro. Antimicrob Agents Chemother. 2002;46(2):425–433