1. Anti-infection Cell Cycle/DNA Damage
  2. HIV Reverse Transcriptase Nucleoside Antimetabolite/Analog
  3. AzddMeC

AzddMeC  (Synonyms: CS-92)

目录号: HY-105268 纯度: 98.96%
COA 产品使用指南

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)。

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AzddMeC Chemical Structure

AzddMeC Chemical Structure

CAS No. : 87190-79-2

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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 EC50 values of AzddMeC are 9 nM and 6 nM, respectively[1][2]. AzddMeC is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.

IC50 & Target[1]

HIV-2

 

HIV-1

9 nM (EC50, Human PBM cells)

HIV-1

6 nM (EC50, Human macrophages)

体外研究
(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)[1].

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

体内研究
(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%[2].

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

分子量

266.26

Formula

C10H14N6O3

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

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

溶解性数据
In Vitro: 

DMSO 中的溶解度 : 200 mg/mL (751.15 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.7557 mL 18.7786 mL 37.5573 mL
5 mM 0.7511 mL 3.7557 mL 7.5115 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.7557 mL 18.7786 mL 37.5573 mL 93.8932 mL
5 mM 0.7511 mL 3.7557 mL 7.5115 mL 18.7786 mL
10 mM 0.3756 mL 1.8779 mL 3.7557 mL 9.3893 mL
15 mM 0.2504 mL 1.2519 mL 2.5038 mL 6.2595 mL
20 mM 0.1878 mL 0.9389 mL 1.8779 mL 4.6947 mL
25 mM 0.1502 mL 0.7511 mL 1.5023 mL 3.7557 mL
30 mM 0.1252 mL 0.6260 mL 1.2519 mL 3.1298 mL
40 mM 0.0939 mL 0.4695 mL 0.9389 mL 2.3473 mL
50 mM 0.0751 mL 0.3756 mL 0.7511 mL 1.8779 mL
60 mM 0.0626 mL 0.3130 mL 0.6260 mL 1.5649 mL
80 mM 0.0469 mL 0.2347 mL 0.4695 mL 1.1737 mL
100 mM 0.0376 mL 0.1878 mL 0.3756 mL 0.9389 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
AzddMeC
目录号:
HY-105268
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