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Description: Zalcitabine (trade name Hivid) is a nucleoside analog HIV reverse transcriptase inhibitor (NARTI). It is an antiviral pyrimidine nucleoside analogue effective against HIV replication. 2′,3′-Dideoxycytidine, when activated to its triphosphate, is incorporated into DNA by HIV-1 RT (HIV-1 reverse transcriptase), causing DNA chain termination and viral replication. Zalcitabine was the third antiretroviral to be approved by the Food and Drug Administration (FDA) for the treatment of HIV/AIDS. It is used as part of a combination regimen. Zalcitabine appears less potent than some other nucleoside RTIs, has an inconvenient three-times daily frequency and is associated with serious adverse events. For these reasons it is now rarely used to treat human immunodeficiency virus (HIV), and it has even been removed from pharmacies entirely in some countries.
References: Am J Med. 1990 May 21;88(5B):2S-7S; Acta Oncol. 1997;36(2):199-205.
Related CAS#: 138540-32-6 (Atevirdine mesylate)
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
In vitro activity: It is phosphorylated in T cells and other HIV target cells into its active triphosphate form, ddCTP. This active metabolite works as a substrate for HIV reverse transcriptase, and also by incorporation into the viral DNA, hence terminating the chain elongation due to the missing hydroxyl group. Since zalcitabine is a reverse transcriptase inhibitor it possesses activity only against retroviruses
Cell Assay: Two human cell lines, WiDr (colon) and MCF-7 (breast) were exposed to ddC at 10 microM concentration for various lengths of time (18, 24, 48 and 72 h). On the WiDr cell line the dual effect of concentration and duration of exposure prior to irradiation was investigated. For MCF-7, ddC induced a significant modification of the dose response only with 24 and 48 h preincubation.
Purity ≥98%
COA
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