For research use only.

Catalog No.S1401 Synonyms: GS-1278

16 publications

Tenofovir  Chemical Structure

CAS No. 147127-20-6

Tenofovir (GS-1278) blocks reverse transcriptase and hepatitis B virus infections.

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Selleck's Tenofovir has been cited by 16 publications

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  • The Nucleotide analog reverse-transcriptase inhibitor Tenofovir disoproxil fumarate was added to TZM-bl cells. Cells were inoculated with 0.05 ng mock-exposed and semen-exposed HIV, and 0.5 ng HIV as infectivity-matched control. Infection rates were measured 3 days post infection by measuring β-galactosidase or or 4 days post infection by measuring luciferase activities. The left panels show the mean enzyme activities ± standard deviation derived from triplicate infections. RLU/s: relative light units per second. Middle panels show normalized infection rates in which reporter enzyme activities obtained from infected cells in the absence of inhibitor were set at 100%. The right panels depict the calculated IC50 values. The number above the bar represents the fold-change in the IC50 derived from 0.05 ng semen-exposed relative to 0.05 or 0.5 ng mock-exposed virus infection. Ns, no statistically significant difference; **** p<0.0001; *** p<0.001 (unpaired t-test).

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

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Biological Activity

Description Tenofovir (GS-1278) blocks reverse transcriptase and hepatitis B virus infections.
Features Tenofovir disoproxil fumarate is the prodrug form of tenofovir.
Reverse transcriptase [1]
In vitro

Tenofovir reduces the viral cytopathic effect of HIV-1(IIIB), HIV-2(ROD) and HIV(EHO) with EC50 of 1.15 μg/mL, 1.12 μg/mL and 1.05 μg/mL in MT-4 cells. Tenofovir also reduces the viral cytopathic effect of SIV(mac251) , SIV(B670) ,SHIV(89.6) and SHIV(RTSHIV). [1] Tenofovir is uniquely active against multinucleoside-resistant HIV expressing the Q151M mutation, but shows reduced susceptibility to the T69S insertion mutations. [2] Tenofovir inhibits hepatitis B virus (HBV) activity in HepG2 2.2.15, HepAD38 and HepAD79 cells. [3] Tenofovir (4 μM) completely inhibits the growth of HIVIIIB in MT-2 cells. Tenofovir inhibits synthesis of negative strand strong-stop DNA with IC50 of 9 µM for wild-type RT, 6 µM for M184V RT and 50 µM for K65R RT. [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human MT2 cells NWXYdnBWTnWwY4Tpc44h[XO|YYm= MYG1JIRigXN? NFjpWIlCdnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEBJUVZzIEPCJIlv\mWldHXkJIlvKGi3bXHuJG1VOiClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJJZqenW|LXnu[JVk\WRiY4n0c5BifGirYzDl[oZm[3RiYX\0[ZIhPSCmYYnzJIJ6KFiWVDDhd5NigSxiRVO1NF0xNjBzMzFOwG0> NHW0eFEzODRyOUeyNS=>
human H9 cells MYHGeY5kfGmxbjDhd5NigQ>? MnLxRY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTGlXOSClbHHk[UBHKGm|b3zheIUhOjN|ODDpcoZm[3SnZDDpckBpfW2jbjDIPUBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oII\pdoFtKHKncHzpZ4F1cW:wLDDFR|UxRTBwMESg{txO MXeyNVgxOzR4Mh?=
C3H/3T3 cells MnnWSpVv[3Srb36gZZN{[Xl? MoLlOkBl[Xm| NUjMPWg5UW6qaXLpeIlwdiCxZjDteZJqdmVic3HyZ49u[SC4aYL1d{1qdmS3Y3XkJJRz[W6|Zn;ycYF1cW:wIH;mJI1wfXOnIHXtZpJ6dyCoaXLyc4Jt[XO2IFOzTE8{XDNiY3XscJMh[W[2ZYKgOkBl[Xm|LDDFR|UxRTBwMkOg{txO MVqxPFU2PjJyOR?=
CEM (human leukemia) cells M4HyO2Z2dmO2aX;uJIF{e2G7 NVf5bVExSW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUEmYLUGgLGlKUUJrIHnuJGNGVSBqaIXtZY4hdGW3a3XtbYEqKGOnbHzzMEBGSzVyPUGuNkDPxE1? M4S2U|E1PTh2OUW2
MT-4 cells M4rtfWZ2dmO2aX;uJIF{e2G7 MnjOTY4hfmm2cn:gZY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTGlXNTJiaX6gUXQuPCClZXzsd{whTUN3ME2xMlQh|ryP MljmNVE{Ojd3OEe=
human bone marrow cells NXTwXY9PS3m2b4TvfIlkcXS7IHHzd4F6 M{jTd|I1KGh? M2H4WGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJIJwdmVibXHydo94KGOnbHzzJIFnfGW{IEK0JIhzeyCkeTDCSnUuTSCjc4PhfUwhS0N3ME2zMlUh|ryP NUDuZpB6OjB2M{m2NFk>
C8166 cells NGW2OWZHfW6ldHnvckBie3OjeR?= NYmyR|hKPCCmYYnz Mlq5RY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgNVAxKFSFSVS1NEB4cWymLYT5dIUhUHWvYX6gbY1ufW6xZHXmbYNq\W6leTD2bZJ2eyC2eYDlJFIhWk:GIHnu[oVkfGWmIHnuJGM5OTZ4IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4Yhe3mwY4n0bYEh\m:{bXH0bY9vKGGodHXyJFQh\GG7czDifUBucWO{b4Pjc5Bq[yCjbnHsfZNqeyxiRVO1NF04NjFizszN MkDPNlE5ODN2NkK=
mouse L1210 cells MmDRR5l1d3SxeHnjbZR6KGG|c3H5 M{DFNlQ5KGh? MYPDfZRwe3SjdHnjJIFkfGm4aYT5JIFo[Wmwc4SgcY92e2ViTEGyNVAh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IHPveYx1\XJiY3;1cpRqdmdiYX7hcJl{cXNuIFnDOVA:OTFizszN NH3W[JMzPDZ6NkCxNi=>
human HepG2 cells NELMZ21HfW6ldHnvckBie3OjeR?= Mor3PUBl[Xm| MULBcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDDI[ZBifGm2aYOgRkB3cXK3czDpcoZm[3SnZDDoeY1idiCKZYDHNkBk\WyuczDh[pRmeiB7IHThfZMh[nliTWTUJIF{e2G7LDDJR|UxRTF{LkOg{txO NITOV3UyPzh6OE[2Ni=>
human HeLa cells M37JOmN6fG:2b4jpZ4l1gSCjc4PhfS=> MkfBO|IhcA>? NU\Ge2s3S3m2b4P0ZZRq[yCjY4Tpeol1gSCjZ3HpcpN1KGi3bXHuJGhmVGFiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JINwfWy2ZYKgZ492dnSrbnegZY5idHm|aYOsJGlEPTB;MUeg{txO M1vYUVI1Pjh4MEGy
CHO cells NXzZenV3S3m2b4TvfIlkcXS7IHHzd4F6 M3HGRlEzOCCq MoLXR5l1d3SxeHnjbZR6KGGpYXnud5QhS0iRIHPlcIx{KGGodHXyJFEzOCCqcoOgZpkhS2WubD3UbZRmeiCJbH:gZZN{[XluIFPDOVA:OjFizszN NF7lVlUyQTByMUGwPC=>
MDCK2 cells NYrkeIVbTnWwY4Tpc44h[XO|YYm= MWKxNEDPxE1? NFrXNXpKdmirYnn0bY9vKG:oIHj1cYFvKE2UUEOg[ZhxemW|c3XkJIlvKE2GQ1uyJINmdGy|IHHzd4V{e2WmIHHzJIlv[3KnYYPlJIlvKGmwdILhZ4VtdHWuYYKgR21HKG[udX;y[ZNk\W6lZTDheEAyOCC3TTDifUBEVU[GQTDhd5NigQ>? NEDuO4syPzF5MkOxNS=>
human HepG2 cells NXO2[oNMS3m2b4TvfIlkcXS7IHHzd4F6 NUXZUoUzOTRiZHH5dy=> MUTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDI[ZBIOiClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJINmdGy3bHHyJGRPSSC{ZYDsbYNifGmxbjDh[pRmeiBzNDDkZZl{ NUW5V2toOjB2MEm3NlE>

... Click to View More Cell Line Experimental Data

In vivo Tenofovir (30 mg/kg) completely prevents SIV infection in all macaques without toxicity. Tenofovir treatment reduces plasma viral RNA levels to undetectable, with parallel decreases in the infectivity of plasma and infectious cells in peripheral blood mononuclear cells and cerebrospinal fluid (CSF) and stabilization of CD4+ T-cell numbers. Tenofovir (30 mg/kg, s.c.) completely abrogates HIV infection via intravaginal exposure in pig-tailed macaques. [5]


Animal Research:[1]
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  • Animal Models: Macaques
  • Dosages: 30 mg/kg
  • Administration: Subcutaneously
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 4 mg/mL warmed (13.92 mM)
Water 2 mg/mL (6.96 mM)
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% propylene glycol, 5% Tween 80, 65% D5W
For best results, use promptly after mixing.
30 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 287.21


CAS No. 147127-20-6
Storage powder
in solvent
Synonyms GS-1278
Smiles CC(CN1C=NC2=C(N=CN=C21)N)OCP(=O)(O)O

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04195776 Not yet recruiting Drug: Tenofovir Douche HIV/AIDS|HIV Prevention Johns Hopkins University|National Institute of Allergy and Infectious Diseases (NIAID)|CONRAD December 1 2020 Phase 1
NCT04530630 Not yet recruiting Drug: BIKTARVY 50Mg-200Mg-25Mg Tablet HIV Infections|Renal Transplant Rejection Weill Medical College of Cornell University|Gilead Sciences September 2020 Phase 3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID