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- 详细信息
- 技术资料
- 保存条件:
4°C, sealed storage, away from moisture
- 英文名:
CS-92
- 库存:
货期:1-2天
- 供应商:
MedChemExpress LLC
- CAS号:
87190-79-2
- 规格:
10 mM * 1 mL/1 mg/5 mg/10 mg/25 mg
| 规格: | 10 mM * 1 mL | 产品价格: | ¥2794.0 |
|---|---|---|---|
| 规格: | 1 mg | 产品价格: | ¥954.0 |
| 规格: | 5 mg | 产品价格: | ¥2100.0 |
| 规格: | 10 mg | 产品价格: | ¥3323.0 |
| 规格: | 25 mg | 产品价格: | ¥5738.0 |
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AzddMeC
CAS No. : 87190-79-2
MCE 国际站:AzddMeC
产品活性: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。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)。
研究领域:Anti-infection | Cell Cycle/DNA Damage
作用靶点:HIV | Reverse Transcriptase | Nucleoside Antimetabolite/Analog
In Vitro: 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: 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%.
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