Tenofovir (GS 1278) Disoproxil Fumarate

For research use only.

Catalog No.S1400 Synonyms: Tenofovir DF

17 publications

Tenofovir (GS 1278) Disoproxil Fumarate Chemical Structure

CAS No. 202138-50-9

Tenofovir Disoproxil Fumarate (GS-1278, Tenofovir DF) 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.

Selleck's Tenofovir (GS 1278) Disoproxil Fumarate has been cited by 17 publications

1 Customer Review

  • 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 (GS 1278) Disoproxil Fumarate purchased from Selleck.

Purity & Quality Control

Choose Selective Reverse Transcriptase Inhibitors

Biological Activity

Description Tenofovir Disoproxil Fumarate (GS-1278, Tenofovir DF) 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 μM and 870 μM, 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 NWX4PYtLTnWwY4Tpc44h[XO|YYm= NXj1UJFuPSCmYYnz MXvJcohq[mm2aX;uJI9nKH[rcoXzMYlv\HWlZXSgZ5l1d3CjdHjpZ{Bm\m[nY4SgbY4hf2muZDD0fZBmKEiLVjCzZUBqdm[nY4Tl[EBOXDJiY3XscJMh[W[2ZYKgOUBl[Xm|LDDFR|UxRTBwMEG1{txO MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzV4MkO2Okc,OTd3NkKzOlY9N2F-
HepG2 M3X0V2N6fG:2b4jpZ4l1gSCjc4PhfS=> NHvvW|M6KGSjeYO= NInoenZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJ\XCJMjDj[YxteyCjZoTldkA6KGSjeYOgZpkhVVSWIHHzd4F6NCCLQ{WwQVIvOzIQvF2= MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzh6OE[2Nkc,OTd6OEi2OlI9N2F-
HepG2 NGrCVGxCdnSrdnnyZYwh[XO|YYm= NGPSdZI6KGSjeYO= NUnDV3RsSW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUGWyYYTpeIl{KEJidnnyeZMhcW6oZXP0[YQhcHWvYX6gTIVxTzJiY3XscJMh[W[2ZYKgPUBl[Xm|IHL5JG1VXCCjc4PhfUwhUUN3ME21MlHPxE1? NG\qXWY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{i4PFY3Oid-MUe4PFg3PjJ:L3G+
MT-2 MmPwRY51cX[rcnHsJIF{e2G7 NXnSRnlbSW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUEmYMTCzRkBqdm[nY4Tl[EBqdiCqdX3hckBOXC1{IHPlcIx{KGK7IIT3c{Bnd2ymIHTpcJV1cW:wIH3leIhw\CCrbjDwdoV{\W6lZTDv[kAyOCViRlLTMEBGSzVyPUCuNFA3QM7:TR?= MlnYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTlzMESwNVAoRjF7MUC0NFExRC:jPh?=
MT2 M3TwcGFvfGm4aYLhcEBie3OjeR?= M1m3OGFvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JGhKXjFiaX7m[YN1\WRiaX6gbJVu[W5iTWSyJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZidnnyZYwhemWybHnjZZRqd25uIFnDOVA:OC53NN88US=> NXTtRVZHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm1PVY5QDVpPkG5OVk3QDh3PD;hQi=>
HeLa P4/R5 NHTWWIpCdnSrdnnyZYwh[XO|YYm= MkLlRY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTGlXOSCrbn\lZ5Rm\CCrbjDoeY1idiCKZVzhJHA1N1J3IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4Yhfmm{YXygdoVxdGmlYYTpc44tKEmFNUC9OE44|ryP Mn[4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl3OU[4PFUoRjF7NUm2PFg2RC:jPh?=
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human bone marrow cells MYXDfZRwfG:6aXPpeJkh[XO|YYm= M{iyVVI1KGi{cx?= MXLDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDic45mKG2jcoLve{Bk\WyuczDh[pRmeiB{NDDodpMh[nliQl\VMWUh[XO|YYmsJGNEPTB;MD65{txO MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODR|OU[wPUc,OjB2M{m2NFk9N2F-
human bone marrow cells M1PVeWN6fG:2b4jpZ4l1gSCjc4PhfS=> M1nSb|I1KGi{cx?= M3LuR2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJIJwdmVibXHydo94KGOnbHzzJIFnfGW{IEK0JIhzeyCkeTDHUU1ETlViYYPzZZktKEOFNUC9NU46|ryP NFjCRpU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MESzPVYxQSd-MkC0N|k3ODl:L3G+
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PBMC NH;L[HBCdnSrdnnyZYwh[XO|YYm= M1vaeVch\GG7cx?= NULuVJVYSW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUEmYMTDpcoZm[3SnZDDpckBpfW2jbjDQRm1EKGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4Yhfmm{YXygdoVxdGmlYYTpc44h[nlibXXhd5VzcW6pIILleoVze2VidILhcpNkemmydHHz[UBi[3Srdnn0fUBqdiClZXzsJJN2eGW{bnH0ZY51KHC{ZXnuZ5Vj[XSnZDD3bZRpKGOnbHzzJIZwdGyxd3XkJIJ6KH[rcnHsJIlv\mWldHnvckBu\WG|dYLl[EBi\nSncjC3JIRigXNiYomgdoFlcW:jY4TpeoUhcW6lLDDFR|UxRTBwMEC0Ou69VQ>? NV7Hd2VsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke0NFU4QTRpPkK3OFA2Pzl2PD;hQi=>
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MT4 MX\BcpRqfmm{YXygZZN{[Xl? M4r1blYh\GG7cx?= NWXuUpF7SW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhfGWwb3\veolzNXKnc3nzeIFvfCCFWFPSOE11em:yaXOgTGlXNTFiTly0MVMhcGG{Yn;ybY5oKHKndnXyd4UhfHKjboPjdolxfGG|ZTDLOlVTKG23dHHueEBqdm[nY4Tl[EBqdiCqdX3hckBOXDRiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kB3cXKjbDDy[ZBtcWOjdHnvckBqdmirYnn0bY9vKG:oII\pdpV{NWmwZIXj[YQh[3m2b4DheIhq[yCnZn\lZ5Qh[W[2ZYKgOkBl[Xm|IHL5JHhVXCCmLDDFR|UxRTFzLkROwG0> Ml\xQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh4OEKwOlcoRjJ6NkiyNFY4RC:jPh?=
HepG2.2.15 M3LaR2FvfGm4aYLhcEBie3OjeR?= NFLBVGFCdnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEBJSlZiaX7m[YN1\WRiaX6gbJVu[W5iSHXwS|IvOi5zNTDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4h[3m2b4DsZZNucWNiRF7BJJN6dnSqZYPpd{BjgSC{ZXXkJIFv\CCvdX7jbEBu\XSqb3SsJGlEPTB;MD64Oe69VQ>? MlzPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzF{MkO0OlAoRjNzMkKzOFYxRC:jPh?=
HepG2.2.15 M3fEWGN6fG:2b4jpZ4l1gSCjc4PhfS=> NGfaXGFEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJ\XCJMj6yMlE2KGOnbHzzJIlv\mWldHXkJJdqfGhiSFLWMEBESzVyPUKwMlcy|ryP M1fJVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzMkKzOFYxLz5|MUKyN|Q3ODxxYU6=

... Click to View More Cell Line Experimental Data

Protocol

Cell Research:

[5]

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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:

[6]

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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)
Water Insoluble
Ethanol ''''44 mg/mL

* 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 Tenofovir DF
Smiles CC(C)OC(=O)OCOP(=O)(COC(C)CN1C=NC2=C(N=CN=C21)N)OCOC(=O)OC(C)C.C(=CC(=O)O)C(=O)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03576066 Completed Drug: ABI-H0731|Drug: SOC NUC|Drug: Placebo Oral Tablet Chronic Hepatitis B Assembly Biosciences June 11 2018 Phase 2
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 --

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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Reverse Transcriptase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID