Tenofovir

Catalog No.S1401 Synonyms: GS-1278

Tenofovir  Chemical Structure

Molecular Weight(MW): 287.21

Tenofovir blocks reverse transcriptase and hepatitis B virus infections.

Size Price Stock Quantity  
In DMSO USD 110 In stock
USD 97 In stock
USD 270 In stock
USD 570 In stock
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Cited by 11 Publications

1 Customer Review

  • 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 blocks reverse transcriptase and hepatitis B virus infections.
Features Tenofovir disoproxil fumarate is the prodrug form of tenofovir.
Targets
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 MXHGeY5kfGmxbjDhd5NigQ>? MVO1JIRigXN? NIrPUllCdnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEBJUVZzIEPCJIlv\mWldHXkJIlvKGi3bXHuJG1VOiClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJJZqenW|LXnu[JVk\WRiY4n0c5BifGirYzDl[oZm[3RiYX\0[ZIhPSCmYYnzJIJ6KFiWVDDhd5NigSxiRVO1NF0xNjBzMzFOwG0> NFrPNoQzODRyOUeyNS=>
human H9 cells NIHydo5HfW6ldHnvckBie3OjeR?= MXXBcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDDITXYyKGOuYXTlJGYhcXOxbHH0[UAzOzN6IHnu[oVkfGWmIHnuJIh2dWGwIFi5JINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZidnnyZYwhemWybHnjZZRqd25uIFXDOVA:OC5yNDFOwG0> NUXJd3YxOjF6MEO0OlI>
C3H/3T3 cells MUXGeY5kfGmxbjDhd5NigQ>? NYixVoVLPiCmYYnz M2rZZWlvcGmkaYTpc44hd2ZibYXybY5mKHOjcnPvcYEhfmm{dYOtbY5lfWOnZDD0doFve2[xcn3heIlwdiCxZjDtc5V{\SCnbXLyfY8h\mmkcn;icIF{fCCFM1ivN3Q{KGOnbHzzJIFnfGW{IE[g[IF6eyxiRVO1NF0xNjJ|IN88US=> MnXCNVg2PTZ{MEm=
CEM (human leukemia) cells M2S2OGZ2dmO2aX;uJIF{e2G7 MmPlRY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTGlXNTFiKFnJTWIqKGmwIFPFUUApcHWvYX6gcIV2c2WvaXGpJINmdGy|LDDFR|UxRTFwMjFOwG0> NH\MXIgyPDV6NEm1Oi=>
MT-4 cells NEOz[41HfW6ldHnvckBie3OjeR?= MlK0TY4hfmm2cn:gZY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTGlXNTJiaX6gUXQuPCClZXzsd{whTUN3ME2xMlQh|ryP NWnnTYNzOTF|Mke1PFc>
human bone marrow cells M{HQXWN6fG:2b4jpZ4l1gSCjc4PhfS=> NWizWVM3OjRiaB?= M4qyUWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJIJwdmVibXHydo94KGOnbHzzJIFnfGW{IEK0JIhzeyCkeTDCSnUuTSCjc4PhfUwhS0N3ME2zMlUh|ryP M1Lkd|IxPDN7NkC5
C8166 cells NH\PfnlHfW6ldHnvckBie3OjeR?= MmDaOEBl[Xm| NX7KNXdQSW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhOTByIGTDTWQ2OCC5aXzkMZR6eGViSIXtZY4hcW2vdX7v[IVncWOrZX7jfUB3cXK3czD0fZBmKDJiUl;EJIlv\mWldHXkJIlvKEN6MU[2JINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2Zic4nuZ5l1cWFiZn;ycYF1cW:wIHHmeIVzKDRiZHH5d{BjgSCvaXPyc5Nkd3CrYzDhcoFtgXOrczygSWM2OD15LkGg{txO MlT0NlE5ODN2NkK=
mouse L1210 cells MYDDfZRwfG:6aXPpeJkh[XO|YYm= NUHZenJnPDhiaB?= M2LrcGN6fG:|dHH0bYMh[WO2aY\peJkh[WejaX7zeEBud3W|ZTDMNVIyOCClZXzsd{Bi\nSncjC0PEBpenNiYomgZ492dHSncjDjc5VvfGmwZzDhcoFtgXOrczygTWM2OD1zMTFOwG0> NXzxVIQ{OjR4OE[wNVI>
human HepG2 cells MUnGeY5kfGmxbjDhd5NigQ>? NVHJZ4wxQSCmYYnz NHj5SHZCdnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEBJ\XCjdHn0bZMhSiC4aYL1d{Bqdm[nY4Tl[EBpfW2jbjDI[ZBIOiClZXzsd{Bi\nSncjC5JIRigXNiYomgUXRVKGG|c3H5MEBKSzVyPUGyMlMh|ryP MorXNVc5QDh4NkK=
human HeLa cells M3O2eGN6fG:2b4jpZ4l1gSCjc4PhfS=> NILKbVg4OiCq MmHyR5l1d3O2YYTpZ{Bi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjlUIEh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IHPveYx1\XJiY3;1cpRqdmdiYX7hcJl{cXNuIFnDOVA:OTdizszN M1zub|I1Pjh4MEGy
CHO cells MkXYR5l1d3SxeHnjbZR6KGG|c3H5 NXz4VGVnOTJyIHi= NEXFemlEgXSxdH;4bYNqfHliYXfhbY5{fCCFSF:gZ4VtdHNiYX\0[ZIhOTJyIHjyd{BjgSCFZXzsMXRqfGW{IFfsc{Bie3OjeTygR2M2OD1{MTFOwG0> NInWZmwyQTByMUGwPC=>
MDCK2 cells NIHlSYZHfW6ldHnvckBie3OjeR?= MkjtNVAh|ryP NHniO5FKdmirYnn0bY9vKG:oIHj1cYFvKE2UUEOg[ZhxemW|c3XkJIlvKE2GQ1uyJINmdGy|IHHzd4V{e2WmIHHzJIlv[3KnYYPlJIlvKGmwdILhZ4VtdHWuYYKgR21HKG[udX;y[ZNk\W6lZTDheEAyOCC3TTDifUBEVU[GQTDhd5NigQ>? Ml:4NVcyPzJ|MUG=
human HepG2 cells MWrDfZRwfG:6aXPpeJkh[XO|YYm= M3juVFE1KGSjeYO= MYfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDI[ZBIOiClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJINmdGy3bHHyJGRPSSC{ZYDsbYNifGmxbjDh[pRmeiBzNDDkZZl{ M2jJTVIxPDB7N{Kx

... 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]

Protocol

Animal Research:[1]
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  • Animal Models: Macaques
  • Formulation: Saline
  • 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
Formula

C9H14N5O4P

CAS No. 147127-20-6
Storage powder
in solvent
Synonyms GS-1278

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04077151 Not yet recruiting Behavioral: PrEP Demonstration Project HIV/AIDS|Gender|Behavior and Behavior Mechanisms Hektoen Institute for Medical Research|National Institute of Mental Health (NIMH) January 1 2020 Not Applicable
NCT04016233 Not yet recruiting Drug: Tenofovir douche HIV/AIDS|HIV Prevention Johns Hopkins University|National Institute of Allergy and Infectious Diseases (NIAID)|University of Pittsburgh December 2019 Phase 1
NCT04065347 Not yet recruiting Device: Digital Pill HIV/AIDS|Adherence Medication University of Colorado Denver|National Institute of Allergy and Infectious Diseases (NIAID) October 2019 --

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Reverse Transcriptase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID