AzddMeC  ≥95%

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包装规格:1mg 5mg in glass bottle
产品简介: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 是一种点击化学试剂。它含有 Azide 基团,可以和含有 Alkyne 基团的分子发生铜催化的叠氮-炔环加成反应(CuAAc)。还可以和含有 DBCO 或 BCN 基团的分子发生菌株促进的炔-叠氮环加成反应 (SPAAC)。
溶解性:DMSO : 200 mg/mL (751.15 mM; 超声助溶)
储备液保存:-80°C, 6 months -20°C, 1 month (sealed storage, away from moisture)
靶点:HIV-2 HIV-1:9 nM (EC50, Human PBM cells) HIV-1:6 nM (EC50, Human macrophages)
体外研究: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).
体内研究: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%.
保存条件:-20℃
注意事项:1、为了您的安全和健康,请穿实验服并戴一次性手套操作。 2、以上信息仅做参考交流之用。