Tenofovir Disoproxil Fumarate

For research use only.

Catalog No.S1400 Synonyms: GS-1278 Disoproxil Fumarate

16 publications

Tenofovir Disoproxil Fumarate Chemical Structure

CAS No. 202138-50-9

Tenofovir (GS-1278) Disoproxil Fumarate belongs to a class of antiretroviral drugs, it inhibits the activity of HIV reverse transcriptase by competing with the natural substrate deoxyadenosine 5’-triphosphate and, after incorporation into DNA, by DNA chain termination.

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10mM (1mL in DMSO) USD 130 In stock
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USD 310 In stock
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Selleck's Tenofovir Disoproxil Fumarate has been cited by 16 publications

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  • Human PBMCs containing indicated concentrations of Tenofovir disoproxil fumarate were inoculated with 5 ng mock-exposed or semen-exposed R5-HIV-luciferase, or 50 ng R5-HIV-luciferase as infectivity matched control. Infection rates were determined 3 days post inoculation.

    Sci Transl Med, 2014, 6(262): 262ra157 . Tenofovir Disoproxil Fumarate purchased from Selleck.

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Biological Activity

Description Tenofovir (GS-1278) Disoproxil Fumarate belongs to a class of antiretroviral drugs, it inhibits the activity of HIV reverse transcriptase by competing with the natural substrate deoxyadenosine 5’-triphosphate and, after incorporation into DNA, by DNA chain termination.
HIV reverse transcriptase [1]
(Cell-free assay)
In vitro

Tenofovir is eliminated from systemic circulation renally through a combination of glomerular filtration and active tubular secretion. Tenofovir is not a substrate for human organic cation transporter type 1 (hOCT1) or hOCT2. Tenofovir accumulates to fivefold lower levels in MRP4-overexpressing cells, and its accumulation could be increased by an MRP inhibitor. [1] Tenofovir produces no significant changes in mitochondrial DNA (mtDNA) levels in human hepatoblastoma (HepG2) cells, skeletal muscle cells (SkMCs), or renal proximal tubule epithelial cells. Tenofovir elevates lactate production by less than 20% in HepG2 cells or SkMCs. [2] Tenofovir is efficiently phosphorylated to tenofovir diphosphate (TFV-DP) in both HepG2 cells and primary human hepatocytes. Tenofovir has a 50% effective concentration of 1.1 mM against HBV in cell-based assays, and potency is improved > 50-fold by the addition of bis-isoproxil progroups. Tenofovir has previously demonstrated full activity against lamivudine-resistant HBV in vitro and clinically. [3] Tenofovir inhibits the proliferation of liver-derived HepG2 cells and normal skeletal muscle cells with CC(50) values of 398 mM and 870 mM, respectively. Tenofovir shows substantially weaker effects on proliferation and viability of renal proximal tubule epithelial cells than cidofovir, a related nucleotide analog with the potential to induce renal tubular dysfunction. [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MT2 cells MVPGeY5kfGmxbjDhd5NigQ>? NFGyTnA2KGSjeYO= Mkm3TY5pcWKrdHnvckBw\iC4aYL1d{1qdmS3Y3XkJIN6fG:yYYTobYMh\W[oZXP0JIlvKHerbHSgeJlx\SCKSW[gN4EhcW6oZXP0[YQhVVR{IHPlcIx{KGGodHXyJFUh\GG7czygSWM2OD1yLkCxOUDPxE1? NV35VIg2OTd3NkKzOlY>
MT2 cells Mk\ZSpVv[3Srb36gZZN{[Xl? NWnle5g3SW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUEmYMTDpcoZm[3SnZDDpckBpfW2jbjDNWFIh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjD2bZJidCC{ZYDsbYNifGmxbjygTWM2OD1yLkW0JO69VQ>? NH25bGkyQTV7Nki4OS=>
human bone marrow cells NHjrc3BEgXSxdH;4bYPDqGG|c3H5 MmnsNlQhcA>? MknZR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gZo9v\SCvYYLyc5ch[2WubIOgZYZ1\XJiMkSgbJJ{KGK7IFLGWU1GKGG|c3H5MEBESzVyPUCuPUDPxE1? NGDKTmMzODR|OU[wPS=>
human HepG2 cells NEXmbIpEgXSxdH;4bYPDqGG|c3H5 MkG5PUBl[Xm| NVywPVRuS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUGWyR{KgZ4VtdHNiYX\0[ZIhQSCmYYnzJIJ6KE2WVDDhd5NigSxiSVO1NF0zNjNzIN88US=> M2r6S|E4QDh6Nk[y
human HeLa P4/R5 cells NHS5bmZHfW6ldHnvckBie3OjeR?= NV25Xo9NSW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUEmYMTDpcoZm[3SnZDDpckBpfW2jbjDI[WxiKFB2L2K1JINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZidnnyZYwhemWybHnjZZRqd25uIFnDOVA:PC55IN88US=> M1fNdVE6PTl4OEi1
human HeLa P4/R5 cells NV7wWIdxTnWwY4Tpc44h[XO|YYm= NIrG[lZCdnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEBJUVZzIHjhdoJwemmwZzDy[ZZmenOnIITyZY5{[3KrcIThd4UhUzZ3UjDteZRidnRiaX7m[YN1\WRiaX6gbJVu[W5iSHXMZUBRPC:UNTDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKH[rcnHsJJJmeGyrY3H0bY9vNCCLQ{WwQVEyNjRizszN MoCwNVk2QTZ6OEW=
human HeLaT4 cells M3fMUmN6fG:2b4jpZ:Kh[XO|YYm= NWLPR|hSS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUGWOYWS0JINmdGy|IHL5JHdUXC1zIHHzd4F6NCCFQ{WwQVM1KM7:TR?= Mn2xNlExPjBzMEi=

... Click to View More Cell Line Experimental Data


Cell Research:


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  • Cell lines: VK2 cells
  • Concentrations: 450 μM or 1,350 μM
  • Incubation Time: 15 min to 12 h
  • Method:

    VK2 cells were exposed to TDF (90 μM or 450 μM) and TFV (450 μM or 1,350 μM) in serum-free RPMI 1640 at 37°C for 15 min to 12 h. At different times postexposure, cells were washed with ice-cold PBS and metabolites were extracted overnight in 70% (vol/vol) methanol, followed by centrifugation at 18,000 × g for 10 min at 4°C. 

    (Only for Reference)
Animal Research:


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  • Animal Models: BALB/c mice
  • Dosages: 50, 500, or 1000 mg/kg
  • Administration: oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (157.35 mM)
Ethanol 44 mg/mL (69.23 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 635.51


CAS No. 202138-50-9
Storage powder
in solvent
Synonyms GS-1278 Disoproxil Fumarate

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03361956 Completed Drug: JNJ-56136379|Drug: Placebo|Drug: NA (ETV or TDF) Hepatitis B Janssen Sciences Ireland UC February 13 2018 Phase 2
NCT02985996 Completed Drug: Truvada|Drug: Genvoya HIV Infections Emory University|Centers for Disease Control and Prevention February 6 2017 Phase 1
NCT03043326 Recruiting Drug: Tenofovir Disoproxil Fumarate and Emtricitabine HIV Prevention Asociación Civil Impacta Salud y Educación Peru|Gilead Sciences January 23 2017 --
NCT01902472 Completed -- HIV Gilead Sciences September 2 2013 --

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Reverse Transcriptase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID