| 包装: | 2.5mg |
| 规格: | 98% |
| 市场价: | 3333元 |
| 分子量: | 277.2 |
Background:
Adefovir-d4is intended for use as an internal standard for the quantification of adefovir by GC- or LC-MS. Adefovir is an active metabolite of the antiviral nucleoside analog adefovir dipivoxil .1Adefovir is formed from adefovir dipivoxil by gastrointestinal carboxylesterase 2 (CES2).2It inhibits cytopathogenicity induced by herpes simplex virus 1 (HSV-1) and HSV-2 (EC50= 7 µg/ml for both in E6SM cells), HIV-1 and HIV-2 (EC50s = 1.8 and 2.5 µg/ml, respectively, in CEM cells), and varicella zoster virus (VZV; EC50= 10 µg/ml in human embryonic lung fibroblasts).3Adefovir (50 mg/kg, p.o.) reduces increases in lymph node viral DNA and serum IgG levels in a mouse model of AIDS induced by infection with the retroviral complex LP-BM5.4It also inhibits tumor growth induced by Moloney sarcoma virus (MSV) infection in mice at the same dose.5
1.Arimilli, M.N., Dougherty, J.P., Cundy, K.C., et al.Orally bioavailable acyclic nucleoside phosphonate prodrugs: Adefovir dipivoxil and bis(POC)PMPAAdvances in Antiviral Drug Design369-91(1999) 2.Laizure, S.C., Herring, V., Hu, Z., et al.The role of human carboxylesterases in drug metabolism: Have we overlooked their importance•Pharmacotherapy33(2)210-222(2013) 3.HolÝ, A., Votruba, I., MasojÍdkovÁ, M., et al.6-[2-(Phosphonomethoxy)alkoxy]pyrimidines with antiviral activityJ. Med. Chem.45(9)1918-1929(2002) 4.Rossi, L., Dominici, S., Serafini, S., et al.Pharmacokinetic and antiretroviral activity in mice of oral [P1,P2-bis[2-(adenin-9-yl)ethoxymethyl]phosphonate], a prodrug of 9-(2-phosphonylmethoxyethyl)adenineJ. Antimicrob. Chemother.50(3)365-374(2002) 5.Naesens, L., Balzarini, J., Bischofberger, N., et al.Antiretroviral activity and pharmacokinetics in mice of oral bis(pivaloyloxymethyl)-9-(2-phosphonylmethoxyethyl)adenine, the bis(pivaloyloxymethyl) ester prodrug of 9-(2-phosphonylmethoxyethyl)adenineAntimicrob. Agents Chemother.40(1)22-28(1996)
m.cnreagent.com