AzddMeC (CS-92) 是一种抗病毒核苷类似物，也是一种有效的，选择性的，具有口服活性的 HIV-1 逆转录酶和 HIV-1 复制的抑制剂。在感染 HIV-1 的人类 PBM 细胞和感染 HIV-1 的人类巨噬细胞中，AzddMeC 的 EC₅₀ 值分别为 9 nM 和 6 nM。

AzddMeC (CS-92) is an antiviral nucleoside analogue and a potent potent, selective and orally active HIV-1 reverse transcriptase and HIV-1 replication inhibitor. In HIV-1-infected human PBM cells and HIV-1-infected human macrophages, the EC 50 values of AzddMeC are 9 nM and 6 nM, respectively.

Solid

HIV-1 9 nM (EC50, Human PBM cells) HIV-1 6

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). has not independently confirmed the accuracy of these methods. They are for reference only.

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%. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

[1]. R F Schinazi, et al. Antiretroviral Activity, Biochemistry, and Pharmacokinetics of 3-azido-2,3-dideoxy-5-methylcytidine. Ann N Y Acad Sci. 1990;616:385-97.
[2]. Boudinot FD, et al. Pharmacokinetics and metabolism of 3-azido-2,3-dideoxy-5-methylcytidine in rhesus monkeys. Drug Metab Dispos. 1993;21(5):855‐860.

In Vitro: DMSO : 200 mg/mL (751.15 mM; Need ultrasonic)配制储备液