CAS NO: | 87190-79-2 |
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] |
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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
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