| Description | AzddMeC (Az-Dcme) is a nucleoside analog with antiviral activity and is an orally active and selective inhibitor of HIV-1 reverse transcriptase and HIV-1 replication.AzddMeC has an EC50 value of 9 nM against HIV-1-infected human PBM cells and 6 nM against HIV-1-infected human macrophages. |
| In vitro | AzddMeC成为乙型肝炎病毒DNA聚合酶最有效的抑制剂（50%抑制剂量，0.03-0.35μM）。相比之下，细胞DNA聚合酶被证明对AzddMeC具有抗性或部分受（β）影响。[4] |
| In vivo | 在对雄性恒河猴静脉内和口服给予 60 mg/kg AzddMeC后，3'-叠氮基-3'-脱氧胸苷(AZT)被发现是猴子AzddMeC的主要代谢产物。血清中的AzddMeC浓度以双指数方式迅速下降，终末半衰期为0.5至1.3小时。AzddMeC 的总清除率为 2.00 +/- 0.41 升/小时/千克（平均值 +/- 标准差），代谢为 AZT 的 AzddMeC 分数为 0.32 +/- 0.05。[2] |
| Target activity | HIV-1:6 nM (EC50, Human macrophages), HIV-1:9 nM (EC50, Human PBM cells) |
| Synonyms | Azidodideoxymethylcytidine, CS-92, Az-Dcme |
| molecular weight | 266.26 |
| Molecular formula | C10H14N6O3 |
| CAS | 87190-79-2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 100 mg/mL (375.57 mM), Sonication is recommended. |
| References | 1. Schinazi RF, et al. Early detection of mixed mutations selected by antiretroviral agents in HIV-infected primary human lymphocytes. Antivir Chem Chemother. 2001;12 Suppl 1:61-5. 2. Boudinot FD, et al. Pharmacokinetics and metabolism of 3'-azido-2',3'-dideoxy-5-methylcytidine in rhesus monkeys. Drug Metab Dispos. 1993 Sep-Oct;21(5):855-60. 3. Cretton EM, et al.Catabolic disposition of 3'-azido-2',3'-dideoxyuridine in hepatocytes with evidence of azido reduction being a general catabolic pathway of 3'-azido-2',3'-dideoxynucleosides. Biochem Pharmacol. 1992 Sep 1;44(5):973-80. 4. Matthes E, et al.Comparative inhibition of hepatitis B virus DNA polymerase and cellular DNA polymerases by triphosphates of sugar-modified 5-methyldeoxycytidines and of other nucleoside analogs. Antimicrob Agents Chemother. 1991 Jun;35(6):1254-7. |