Name | AzddMeC |
Synonyms | CS-92 AzddMeC Az-Dcme Azidodideoxymethylcytidine 3'-azido-2',3'-dideoxy-5-methylcytidine 3'-Azido-2',3'-dideoxy-4-deoxo-4-imino-5-methyluridine |
CAS | 87190-79-2 |
Molecular Formula | C10H14N6O3 |
Molar Mass | 266.26 |
Storage Condition | -20°C,密封,干燥 |
In vitro study | AzddMeC (CS-92) is also effective against HIV-2 in lymphocytes. The replication of Friend murine virus is only weakly inhibited, and no effect is observed against HSV type 1 and type 2 and coxsackievirus B4. The interaction of the 5'-triphosphate of AzddMeC with HIV-1 reverse transcriptase indicated competitive inhibition (the inhibition constant, Kis, is 9.3 nM). |
In vivo study | The pharmacokinetics of AzddMeC are characterized following intravenous and oral administration of 60 mg/kg of the compound to male rhesus monkeys. 3'-azido-3'-deoxythymidine (AZT) is a major metabolite of AzddMeC in monkeys. AzddMeC concentrations in serum declined rapidly in a biexponential fashion with the terminal half-life ranging from 0.5 to 1.3 hr. Renal excretion of unchanged nucleoside and metabolic deamination yielding AZT are the primary routes of AzddMeC clearance. The oral bioavailability is 26%. |
biological activity | AzddMeC (CS-92) is an antiviral nucleoside analog that is also a potent, selective, inhibitor of HIV-1 reverse transcriptase and HIV-1 replication with oral activity. The EC50 values of AzddMeC were 9 nM and 6 nM in HIV-1 infected human PBM cells and HIV-1 infected human macrophages, respectively. |