SKU: T128  / 
    CAS Number: 379270-37-8

    Tenofovir Alafenamide

    $135.45 - $183.75
    Tenofovir alafenamide is an antiretroviral developed by Gilead and the anti-HIV  activity was reported  in 1993.  It is an investigational precursor to Tenovor, a nucleotide reverse transcriptase inhibitor.  Tenofovir alafenamide is more efficient at delivering Tenofovir to target cells.
    Mechanism of ActionTenofovir alafenamide is a nucleotide analog reverse transcriptase inhibitor that terminates DNA transcription.
    Eukaryotic Cell Culture ApplicationsTenofovir alafenamide is 1000- and 10-fold more active against HIV in vitro than Tenofovir or tenofovir disoproxil fumarate, respectively, and the compound is stable in biological matrices (Ray et al, 2016). It reduces HIV-1 viral replication in MT-2 cells with an EC50 value of 5 nM (Ray et al, 2016). During in vitro studies with activated or resting peripheral blood mononuclear cells, MT2 and Jerkat T-cell lines, authors found that Tenofovir alafenamide did not inhibit mitochondrial DNA synthesis (Stray et al, 2017).
    Molecular FormulaC21H29N6O5P
    Solubilityfreely soluble in methanol,soluble in ethanol and DMSO, sparingly soluble in water.
    ReferencesBalzarini J et al (1993) Differential antiherpesvirus and antiretrovirus effects of the (S) and (R) enantiomers of acyclic nucleoside phosphonates: potent and selective in vitro and in vivo antiretrovirus activities of (R)-9-(2-phosphonomethoxypropyl)-2,6-diaminopurine Antimicrob. Agents Chemother. 37:332-338 PMID 8452366 Lee WA (2005) Selective intracellular activation of a novel prodrug of the human immunodeficiency virus reverse transcriptase inhibitor tenofovir leads to preferential distribution and accumulation in lymphatic tissue.Antimicrob Agents Chemother. 49(5):1898-1906 PMID 15855512 Ray AS, Fordyce MW, and Hitchcock MJM (2016) Tenofovir alafenamide: A novel prodrug of tenofovir for the treatment of human immunodeficiency virus. Antiviral Res. 125:63-70 Stray KM et al (2017) Tenofovir alafenamide (TAF) does not deplete mitochondrial DNA in human T-cell lines at intracellular concentrations exceeding clinically relevant drug exposures. Antiviral Res. 140:116-120