87190-79-2

中文名称 3'-叠氮基-2',3'-二脱氧-5-甲基胞苷

英文名称 3'-azido-2',3'-dideoxy-5-methylcytidine

CAS 87190-79-2

分子式 C10H14N6O3

分子量 266.26

MOL 文件 87190-79-2.mol

更新日期 2023/03/20 15:41:21

87190-79-2 结构式

基本信息物理化学性质常见问题列表

基本信息

中文别名

3'-叠氮基-2',3'-二脱氧-5-甲基胞苷

英文别名

CS-92
AzddMeC
3'-azido-2',3'-dideoxy-5-methylcytidine
3'-Azido-2',3'-dideoxy-4-deoxo-4-imino-5-methyluridine

物理化学性质

储存条件4°C, away from moisture

溶解度DMSO : 200 mg/mL (751.15 mM; Need ultrasonic)

形态Solid

颜色White to off-white

常见问题列表

生物活性

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。

靶点

HIV-1

9 nM (EC ₅₀ , Human PBM cells)

HIV-1

6 nM (EC ₅₀ , 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%.