Tenofovir Disoproxil Fumarate

Catalog No.S1400 Synonyms: GS-1278 Disoproxil Fumarate

Tenofovir Disoproxil Fumarate Chemical Structure

Molecular Weight(MW): 635.51

Tenofovir 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.

Size Price Stock Quantity  
In DMSO USD 130 In stock
USD 97 In stock
USD 310 In stock
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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 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.
Targets
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 NVzhW5ZxTnWwY4Tpc44h[XO|YYm= NEDVWJQ2KGSjeYO= M3rLXmlvcGmkaYTpc44hd2ZidnnyeZMucW6mdXPl[EBkgXSxcHH0bIlkKGWoZnXjeEBqdiC5aXzkJJR6eGViSFnWJFNiKGmwZnXjeIVlKE2WMjDj[YxteyCjZoTldkA2KGSjeYOsJGVEPTB;MD6wNVUh|ryP MoK3NVc2PjJ|Nk[=
MT2 cells MlLiSpVv[3Srb36gZZN{[Xl? MU\BcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDDITXYyKGmwZnXjeIVlKGmwIHj1cYFvKE2WMjDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKH[rcnHsJJJmeGyrY3H0bY9vNCCLQ{WwQVAvPTRizszN Mom0NVk2QTZ6OEW=
human bone marrow cells M{DKU2N6fG:2b4jpZ:Kh[XO|YYm= NGHTWHozPCCq NIjuenFEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBjd26nIH3hdpJwfyClZXzsd{Bi\nSncjCyOEBpenNiYomgRmZWNUViYYPzZZktKEOFNUC9NE46KM7:TR?= NUPnRXNNOjB2M{m2NFk>
human HepG2 cells MX;DfZRwfG:6aXRCpIF{e2G7 Mm\lPUBl[Xm| M1XkUWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhmeEd{IHPlcIx{KGGodHXyJFkh\GG7czDifUBOXFRiYYPzZZktKEmFNUC9Nk4{OSEQvF2= MmTaNVc5QDh4NkK=
human HeLa P4/R5 cells NGnFUYJHfW6ldHnvckBie3OjeR?= MmriRY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTGlXOSCrbn\lZ5Rm\CCrbjDoeY1idiCKZVzhJHA1N1J3IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4Yhfmm{YXygdoVxdGmlYYTpc44tKEmFNUC9OE44KM7:TR?= NXXMOnlXOTl3OU[4PFU>
human HeLa P4/R5 cells NIfqNXhHfW6ldHnvckBie3OjeR?= MmqwRY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTGlXOSCqYYLic5JqdmdicnX2[ZJ{\SC2cnHud4NzcXC2YYPlJGs3PVJibYX0ZY51KGmwZnXjeIVlKGmwIHj1cYFvKEinTHGgVFQwWjViY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kB3cXKjbDDy[ZBtcWOjdHnvckwhUUN3ME2xNU41KM7:TR?= NWnLOXpiOTl3OU[4PFU>
human HeLaT4 cells NHLvfJNEgXSxdH;4bYPDqGG|c3H5 NFnFXIZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJ\UyjVESgZ4VtdHNiYomgW3NVNTFiYYPzZZktKEOFNUC9N|Qh|ryP Mk\YNlExPjBzMEi=

... Click to View More Cell Line Experimental Data

Protocol

Cell Research:

[5]

+ Expand
  • 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:

[6]

+ Expand
  • Animal Models: BALB/c mice
  • Formulation: 50 mM trisodium citrate dihydrate
  • 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
Formula

C19H30N5O10P.C4H4O4

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

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03251144 Recruiting HIV/AIDS|Antiviral Toxicity|Antiviral Drug Adverse Reaction|Mitochondrial Alteration University of California Los Angeles|Gilead Sciences September 8 2018 Phase 1|Phase 2
NCT02431247 Active not recruiting Immunodeficiency Virus Type 1 Human Janssen Sciences Ireland UC July 6 2015 Phase 3
NCT01721109 Completed Acquired Immunodeficiency Syndrome|HIV Infections Gilead Sciences December 6 2012 Phase 2|Phase 3
NCT01480622 Completed Hepatitis B Chronic GlaxoSmithKline December 5 2011 Phase 1
NCT03032536 Terminated Hepatitis B|Chronic Hepatitis B|Viral Hepatitis B Alios Biopharma Inc. January 31 2017 Phase 1
NCT03547908 Recruiting HIV-1/HBV Co-Infection Gilead Sciences May 30 2018 Phase 3

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Reverse Transcriptase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID