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AzddMeC
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
AzddMeC图片
CAS NO:87190-79-2

CS-92
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。
生物活性

AzddMeC (CS-92) is an antiviralnucleoside analogueand a potent potent, selective and orally activeHIV-1reverse transcriptaseandHIV-1replicationinhibitor. InHIV-1-infected human PBM cells andHIV-1-infected human macrophages, theEC50values of AzddMeC are 9 nM and 6 nM, respectively[1][2].

IC50& Target[1]

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].

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].

分子量

266.26

性状

Solid

Formula

C10H14N6O3

CAS 号

87190-79-2

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

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM3.7557 mL18.7786 mL37.5573 mL
5 mM0.7511 mL3.7557 mL7.5115 mL
10 mM0.3756 mL1.8779 mL3.7557 mL
*

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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

 
 
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