AzddMeC (Synonyms: CS-92) |
Catalog No.GC65963 |
AzddMeC(CS-92)는 항바이러스 뉴클레오시드 유사체이며 강력하고 선택적인 경구 활성 HIV-1 역전사효소 및 HIV-1 복제 억제제입니다. 821d96072c2d58d8970e76f526b0f6b8HIV-1에 감염된 인간 PBM 세포와 HIV-1에 감염된 인간 대식세포에서 AzddMeC의 EC50 값은 각각 9nM과 6nM입니다.821d96072c2d58d8970e76f526b0f6b8
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Cas No.: 87190-79-2
Sample solution is provided at 25 µL, 10mM.
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 (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].
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].
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