87190-79-2
基本信息
AzddMeC
3'-azido-2',3'-dideoxy-5-methylcytidine
3'-Azido-2',3'-dideoxy-4-deoxo-4-imino-5-methyluridine
物理化學(xué)性質(zhì)
常見問題列表
HIV-1 9 nM (EC 50 , Human PBM cells) |
HIV-1 6 nM (EC 50 , Human macrophages) |
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).
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%.