AdefovirAdefovir
MedChemExpress (MCE)
HY-B1826
106941-25-7
GS-0393
PMEA
99.55%
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Room temperature in continental US
may vary elsewhere.
Adefovir (GS-0393) is an adenosine monophosphate analog antiviral agent that after intracellular conversion to Adefovir diphosphate inhibits HBV DNA polymerase. Adefovir has an IC50 of 0.7 μM against HBV in the HepG2.2.15 cell line. Adefovir has good antiviral activity against several viruses, including HBV and herpesviruses.
Studies to elucidate the mechanism of action of Adefovir against herpesvirus replication reveals that the phosphorylation of Adefovir occurred intracellularly and is carried out by host cellular enzymes. The diphosphorylated derivatives of Adefovir targeted the viral DNA polymerase and also acted as DNA chain terminators. Adenylate kinase is shown to be responsible for the first phosphorylation, which was followed by ADP kinase and creatine kinase, forming Adefovir diphosphate[1].
Unaffected by food, Adefovir achieves 60% oral bioavailability. Its half-life is 12-30 hours and Adefovir undergoes renal excretion without significant metabolites. Adefovir does not substantially affect the cytochrome P450 system[3].
HBV[1][2][3]
DNA polymerase[1][2] Cellular Effect Cell Line Type Value Description References
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[1]. X.-X.Zhou, et al. 7.11 - Deoxyribonucleic Acid Viruses: Antivirals for Herpesviruses and Hepatitis B Virus. Comprehensive Medicinal Chemistry II. Volume 7, 2007, Pages 295-327.
[2]. Marcellin P, et al. Adefovir dipivoxil for the treatment of hepatitis B e antigen-positive chronic hepatitis B. N Engl J Med. 2003 Feb 27
348(9):808-16. [Content Brief]
[3]. Leah A.Burke, et al. 155 - Drugs to Treat Viral Hepatitis. Infectious Diseases. Volume 2, 2017, Pages 1327-1332.