Tenofovir (GS 1278) Disoproxil Fumarate

Catalog No.S1400 Synonyms: Tenofovir DF

For research use only.

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.

Tenofovir (GS 1278) Disoproxil Fumarate Chemical Structure

CAS No. 202138-50-9

Selleck's Tenofovir (GS 1278) Disoproxil Fumarate has been cited by 21 publications

Purity & Quality Control

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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 MUfGeY5kfGmxbjDhd5NigQ>? MmK5OUBl[Xm| M2nueWlvcGmkaYTpc44hd2ZidnnyeZMucW6mdXPl[EBkgXSxcHH0bIlkKGWoZnXjeEBqdiC5aXzkJJR6eGViSFnWJFNiKGmwZnXjeIVlKE2WMjDj[YxteyCjZoTldkA2KGSjeYOsJGVEPTB;MD6wNVXPxE1? M1y1c|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NU[yN|Y3Lz5zN{W2NlM3PjxxYU6=
HepG2 NELpOVNEgXSxdH;4bYNqfHliYYPzZZk> NVrkbFd5QSCmYYnz NHrYcllEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJ\XCJMjDj[YxteyCjZoTldkA6KGSjeYOgZpkhVVSWIHHzd4F6NCCLQ{WwQVIvOzIQvF2= NYnVO|g5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUe4PFg3PjJpPkG3PFg5PjZ{PD;hQi=>
HepG2 MWXBcpRqfmm{YXygZZN{[Xl? M2r1R|kh\GG7cx?= MoDzRY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTIVx[XSrdHnzJGIhfmm{dYOgbY5n\WO2ZXSgbJVu[W5iSHXwS|Ih[2WubIOgZYZ1\XJiOTDkZZl{KGK7IF3UWEBie3OjeTygTWM2OD13LkJOwG0> M4PoNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5OEi4OlYzLz5zN{i4PFY3OjxxYU6=
MT-2 MWfBcpRqfmm{YXygZZN{[Xl? MX7BcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDDITXYyKDOEIHnu[oVkfGWmIHnuJIh2dWGwIF3UMVIh[2WubIOgZpkhfHexIH\vcIQh\GmudYTpc44hdWW2aH;kJIlvKHC{ZYPlcoNmKG:oIEGwKUBHSlNuIFXDOVA:OC5yME[4{txO MlXyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTlzMESwNVAoRjF7MUC0NFExRC:jPh?=
MT2 M2CxSWFvfGm4aYLhcEBie3OjeR?= MnX4RY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTGlXOSCrbn\lZ5Rm\CCrbjDoeY1idiCPVEKgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iC4aYLhcEBz\XCuaXPheIlwdixiSVO1NF0xNjV2zszN NUXvXHBVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm1PVY5QDVpPkG5OVk3QDh3PD;hQi=>
HeLa P4/R5 NHrxRVlCdnSrdnnyZYwh[XO|YYm= M{G2NWFvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JGhKXjFiaX7m[YN1\WRiaX6gbJVu[W5iSHXMZUBRPC:UNTDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKH[rcnHsJJJmeGyrY3H0bY9vNCCLQ{WwQVQvP87:TR?= M3LFdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7NUm2PFg2Lz5zOUW5Olg5PTxxYU6=
HeLa P4/R5 MYTBcpRqfmm{YXygZZN{[Xl? M1XRRWFvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JGhKXjFiaHHyZo9zcW6pIILleoVze2VidILhcpNkemmydHHz[UBMPjWUIH31eIFvfCCrbn\lZ5Rm\CCrbjDoeY1idiCKZVzhJHA1N1J3IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4Yhfmm{YXygdoVxdGmlYYTpc44tKEmFNUC9NVEvPM7:TR?= MlPZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl3OU[4PFUoRjF7NUm2PFg2RC:jPh?=
human bone marrow cells MmPmR5l1d3SxeHnjbZR6KGG|c3H5 NHPoe3ozPCCqcoO= NInU[lFEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBjd26nIH3hdpJwfyClZXzsd{Bi\nSncjCyOEBpenNiYomgRmZWNUViYYPzZZktKEOFNUC9NE46|ryP NWW5cIVWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC0N|k3ODlpPkKwOFM6PjB7PD;hQi=>
human bone marrow cells MWTDfZRwfG:6aXPpeJkh[XO|YYm= NI[2SG4zPCCqcoO= MYjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDic45mKG2jcoLve{Bk\WyuczDh[pRmeiB{NDDodpMh[nliR12tR2ZWKGG|c3H5MEBESzVyPUGuPe69VQ>? NVHFenFGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC0N|k3ODlpPkKwOFM6PjB7PD;hQi=>
HeLa-T4 NFTxeGNCdnSrdnnyZYwh[XO|YYm= NEfpWmc1QCCqcoO= MWTBcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDDzbY5odGVvcn;1coQhUEmYMTDOUHgvVHW6LWKgbIFz[m:{aX7nJIlv[WO2aY\heIlv\yCvdYTheIlwdnNiaX6g[Y53NCC4cIKgZY5lKGOjcoLp[ZMh\mm{ZX\sfUBtfWOrZnXyZZNmKGenbnWgbY4heGyjY3Wgc4YhdmWoIHnu[oVkfGWmIHnuJIh2dWGwIFjlUIEuXDRiY3XscJMh[XO|ZYPz[YQh[XNibIXjbYZmemG|ZTDhZ5Rqfmm2eTDh[pRmeiB2ODDodpMh[nliZYjv[4Vvd3W|IGLUJIF{e2G7LDDFR|UxRTBwMECyPe69VQ>? NXfubWtORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGwOlAyODhpPkKxNFYxOTB6PD;hQi=>
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HeLaT4 M1Xa[2FvfGm4aYLhcEBie3OjeR?= MlfPNlQhcHK| MnnsRY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4Sgd4lv\2ynLYLveY5lKEiLVkGgUmxZNky3eD3SJIhiemKxcnnu[{BqdmGldHn2ZZRqdmdibYX0ZZRqd26|IHnuJIVvfixidoDyJIFv\CClYYLybYV{KG[rcnXmcJkhdHWlaX\ldoF{\SCpZX7lJIlvKHCuYXPlJI9nKG6nZjDhd5Nme3OnZDDhd{Bt\X[nbDDv[kBqdm[nY4Tpc44hfXOrbnegbJVu[W5iSHXMZXQ1KGOnbHzzJJBz\XS{ZXH0[YQh[XRiMUCwJJRqdWViRVO5OUBnd3JiMkSgbJJ{KG[xbHzve4Vl NX;aO2hCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGwOlAyODhpPkKxNFYxOTB6PD;hQi=>
PBMC NWP3RnR6SW62aY\pdoFtKGG|c3H5 MWq3JIRigXN? NXjIdHpxSW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUEmYMTDpcoZm[3SnZDDpckBpfW2jbjDQRm1EKGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4Yhfmm{YXygdoVxdGmlYYTpc44h[nlibXXhd5VzcW6pIILleoVze2VidILhcpNkemmydHHz[UBi[3Srdnn0fUBqdiClZXzsJJN2eGW{bnH0ZY51KHC{ZXnuZ5Vj[XSnZDD3bZRpKGOnbHzzJIZwdGyxd3XkJIJ6KH[rcnHsJIlv\mWldHnvckBu\WG|dYLl[EBi\nSncjC3JIRigXNiYomgdoFlcW:jY4TpeoUhcW6lLDDFR|UxRTBwMEC0Ou69VQ>? NEWyWpU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{SwOVc6PCd-Mke0NFU4QTR:L3G+
HepG2.2.15 MoPORY51cX[rcnHsJIF{e2G7 M{DIXFMh\GG7cx?= NGXYbIpCdnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEBJSlZiaX7m[YN1\WRiaX6gbJVu[W5iSHXwS|IvOi5zNTDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKH[rcnHsJGRPSSCrbjDj[YxtKHO3cHXycoF1[W62IHnuZ5Vj[XSnZDDmc5IhOyCmYYnzJIlvKHC{ZYPlcoNmKG:oIEGwKUBHSlNiZn;scI94\WRiYomgZ49ueG:3bnSgeJJm[XSvZX70JIlvKGGkc3XuZ4Uhd2ZiMUClJGZDWyCob4KgN{Bl[Xm|IHL5JJFTXC2SQ2KgcYV1cG:mLDDFR|UxRTBwM{VOwG0> M4TRVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5NEC1O|k1Lz5{N{SwOVc6PDxxYU6=
HepG2.2.15 MX;DfZRwfG:6aXPpeJkh[XO|YYm= MlfyOkBl[Xm| MlXkR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTIVxTzJwMj6xOUBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkh[W[2ZYKgOkBl[Xm|IHL5JHhVXCCjc4PhfUwhS0N3ME2yPU4z|ryP MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzRyNUe5OEc,Ojd2MEW3PVQ9N2F-
PBMC MkPaRY51cX[rcnHsJIF{e2G7 MnnNN|AhdWmwcx?= Mof5RY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgR3hEWjRvdILvdIlkKEiLVj2xJG5NPC1|IHnu[oVkfGWmIHnuJIh2dWGwIGDIRU1{fGmvdXzheIVlKFCETVOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjD2bZJidCC{ZYDsbYNifGmxbjDifUBu\WG|dYLpcochemWmdXP0bY9vKGmwIICyOEBidnSrZ3XuJJBzd2S3Y4Tpc44heHKnaX7jeYJifGWmIIfpeIgh[2WubIOg[o9zKDNyIH3pcpMh\m:ubH;3[YQh[nlidnnyZYwhcW6oZXP0bY9vKG2nYYP1doVlNCCLQ{WwQVAvODkQvF2= NUnVe2JoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki2PFIxPjdpPkK4OlgzODZ5PD;hQi=>
PBMC M17HWGFvfGm4aYLhcEBie3OjeR?= NH;WS5Y{OCCvaX7z MX3BcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDDDR3I2KHS{b4DpZ{BJUVZzIFLhUEBqdm[nY4Tl[EBqdiCqdX3hckBRUEFvc4TpcZVt[XSnZDDQRm1EKGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4Yhfmm{YXygdoVxdGmlYYTpc44h[nlibXXhd5VzcW6pIILl[JVkfGmxbjDpckBxOjRiYX70bYdmdiCycn;keYN1cW:wIIDy[Ylv[3WkYYTl[EB4cXSqIHPlcIx{KG[xcjCzNEBucW6|IH\vcIxwf2WmIHL5JJZqemGuIHnu[oVkfGmxbjDt[YF{fXKnZDDvckAtKEmFNUC9NE4zOs7:TR?= M1vrSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6NkiyNFY4Lz5{OE[4NlA3PzxxYU6=
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HepG2.2.15 M3zrcGFvfGm4aYLhcEBie3OjeR?= M2LhUGFvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JGhDXiCrbn\lZ5Rm\CCrbjDoeY1idiCKZYDHNk4zNjF3IHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBkgXSxcHzhd41q[yCGTlGgd5lvfGinc3nzJIJ6KHKnZXSgZY5lKG23bnPoJI1mfGixZDygTWM2OD1yLki1{txO MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{OTJ{M{S2NEc,OzF{MkO0OlA9N2F-
HepG2.2.15 MornR5l1d3SxeHnjbZR6KGG|c3H5 MX7DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDI[ZBIOi5{LkG1JINmdGy|IHnu[oVkfGWmIIfpeIghUEKYLDDDR|UxRTJyLkex{txO MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{OTJ{M{S2NEc,OzF{MkO0OlA9N2F-

Protocol (from reference)

Cell Research:

[5]

  • 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. 

Animal Research:

[6]

  • Animal Models: BALB/c mice
  • Dosages: 50, 500, or 1000 mg/kg
  • Administration: oral administration

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 635.51
Formula

C19H30N5O10P.C4H4O4

CAS No. 202138-50-9
Storage 3 years -20°C powder
2 years -80°C in solvent
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)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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 --

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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

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