Tenofovir

Catalog No.S1401 Synonyms: GS-1278

Tenofovir  Chemical Structure

Molecular Weight(MW): 287.21

Tenofovir blocks reverse transcriptase and hepatitis B virus infections.

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In DMSO USD 110 In stock
USD 97 In stock
USD 270 In stock
USD 570 In stock
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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 NHPaNYJHfW6ldHnvckBie3OjeR?= Mn;POUBl[Xm| NHj2NXJCdnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEBJUVZzIEPCJIlv\mWldHXkJIlvKGi3bXHuJG1VOiClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJJZqenW|LXnu[JVk\WRiY4n0c5BifGirYzDl[oZm[3RiYX\0[ZIhPSCmYYnzJIJ6KFiWVDDhd5NigSxiRVO1NF0xNjBzMzFOwG0> NY\sO3NtOjB2MEm3NlE>
human H9 cells M1zsTmZ2dmO2aX;uJIF{e2G7 MkP2RY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTGlXOSClbHHk[UBHKGm|b3zheIUhOjN|ODDpcoZm[3SnZDDpckBpfW2jbjDIPUBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oII\pdoFtKHKncHzpZ4F1cW:wLDDFR|UxRTBwMESg{txO MYCyNVgxOzR4Mh?=
C3H/3T3 cells M{\ST2Z2dmO2aX;uJIF{e2G7 MUO2JIRigXN? NIDTPVZKdmirYnn0bY9vKG:oIH31dolv\SC|YYLjc41iKH[rcoXzMYlv\HWlZXSgeJJidnOob4LtZZRqd25ib3[gcY92e2ViZX3idplwKG[rYoLvZoxie3RiQ{PIM|NVOyClZXzsd{Bi\nSncjC2JIRigXNuIFXDOVA:OC5{MzFOwG0> MoCyNVg2PTZ{MEm=
CEM (human leukemia) cells Mn3tSpVv[3Srb36gZZN{[Xl? MYrBcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDDITXYuOSBqSVnJRkkhcW5iQ1XNJEhpfW2jbjDs[ZVs\W2rYTmgZ4VtdHNuIFXDOVA:OS5{IN88US=> NILNPW8yPDV6NEm1Oi=>
MT-4 cells M{TQSGZ2dmO2aX;uJIF{e2G7 MlTFTY4hfmm2cn:gZY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTGlXNTJiaX6gUXQuPCClZXzsd{whTUN3ME2xMlQh|ryP NInSXlAyOTN{N{W4Oy=>
human bone marrow cells NX\PSmxsS3m2b4TvfIlkcXS7IHHzd4F6 NXq5ZWdGOjRiaB?= NYfMSItiS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4h[m:wZTDtZZJzd3diY3XscJMh[W[2ZYKgNlQhcHK|IHL5JGJHXS2HIHHzd4F6NCCFQ{WwQVMvPSEQvF2= NXLzOHNsOjB2M{m2NFk>
C8166 cells NWfST|g2TnWwY4Tpc44h[XO|YYm= NXj2N2xQPCCmYYnz NFTud2lCdnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEAyODBiVFPJSFUxKHerbHSteJlx\SCKdX3hckBqdW23bn;k[YZq[2mnbnP5JJZqenW|IIT5dIUhOiCUT1SgbY5n\WO2ZXSgbY4hSzhzNk[gZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iC|eX7jfZRq[SCob4LtZZRqd25iYX\0[ZIhPCCmYYnzJIJ6KG2rY4Lvd4NweGmlIHHuZYx6e2m|LDDFR|UxRTdwMTFOwG0> M162S|IyQDB|NE[y
mouse L1210 cells M13Ve2N6fG:2b4jpZ4l1gSCjc4PhfS=> MnvFOFghcA>? M1TGR2N6fG:|dHH0bYMh[WO2aY\peJkh[WejaX7zeEBud3W|ZTDMNVIyOCClZXzsd{Bi\nSncjC0PEBpenNiYomgZ492dHSncjDjc5VvfGmwZzDhcoFtgXOrczygTWM2OD1zMTFOwG0> NXvSRXNmOjR4OE[wNVI>
human HepG2 cells MXTGeY5kfGmxbjDhd5NigQ>? Ml3IPUBl[Xm| NX:zWYpkSW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUGWyYYTpeIl{KEJidnnyeZMhcW6oZXP0[YQhcHWvYX6gTIVxTzJiY3XscJMh[W[2ZYKgPUBl[Xm|IHL5JG1VXCCjc4PhfUwhUUN3ME2xNk4{KM7:TR?= M{f4eFE4QDh6Nk[y
human HeLa cells M3f6cWN6fG:2b4jpZ4l1gSCjc4PhfS=> NHL1fYs4OiCq NWnWWYY2S3m2b4P0ZZRq[yCjY4Tpeol1gSCjZ3HpcpN1KGi3bXHuJGhmVGFiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JINwfWy2ZYKgZ492dnSrbnegZY5idHm|aYOsJGlEPTB;MUeg{txO NEPic4YzPDZ6NkCxNi=>
CHO cells MUfDfZRwfG:6aXPpeJkh[XO|YYm= M{LvZ|EzOCCq NH;F[4lEgXSxdH;4bYNqfHliYXfhbY5{fCCFSF:gZ4VtdHNiYX\0[ZIhOTJyIHjyd{BjgSCFZXzsMXRqfGW{IFfsc{Bie3OjeTygR2M2OD1{MTFOwG0> M3j3UVE6ODBzMUC4
MDCK2 cells MYXGeY5kfGmxbjDhd5NigQ>? MlvVNVAh|ryP NW\3U3B{UW6qaXLpeIlwdiCxZjDoeY1idiCPUmCzJIV5eHKnc4Pl[EBqdiCPRFPLNkBk\WyuczDhd5Nme3OnZDDhd{BqdmO{ZXHz[UBqdiCrboTyZYNmdGy3bHHyJGNOTiCobIXvdoV{[2WwY3WgZZQhOTBidV2gZpkhS02IRFGgZZN{[Xl? M{\uUlE4OTd{M{Gx
human HepG2 cells NVnwVWhYS3m2b4TvfIlkcXS7IHHzd4F6 NUn4cZBHOTRiZHH5dy=> MWLDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDI[ZBIOiClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJINmdGy3bHHyJGRPSSC{ZYDsbYNifGmxbjDh[pRmeiBzNDDkZZl{ MVeyNFQxQTd{MR?=

... 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 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
NCT03126370 Recruiting Hepatitis C|HIV Coinfection University of Colorado Denver January 8 2018 Phase 4
NCT03067285 Recruiting HIV Infections Fundacion SEIMC-GESIDA September 8 2017 Phase 4
NCT03060785 Completed HIV Prevention Johns Hopkins University March 8 2016 Phase 1
NCT03425994 Recruiting Chronic Hepatitis B in HIV Patient|Kidney Injury|Bone Diseases National Taiwan University Hospital|National Taiwan University Hospital Hsin-Chu Branch|National Taiwan University Hospital Yun-Lin Branch|Far Eastern Memorial Hospital|Taoyuan General Hospital|Mackay Memorial Hospital|Chung Shan Medical University|Taichung Veterans General Hospital|National Cheng-Kung University Hospital|Changhua Christian Hospital|Chi Mei Medical Hospital|Kaohsiung Veterans General Hospital.|Kaohsiung Medical University Chung-Ho Memorial Hospital|Chang Gung Memorial Hospital|E-DA Hospital|Lotung Poh-Ai Hospital February 6 2018 --
NCT02431247 Active not recruiting Immunodeficiency Virus Type 1 Human Janssen Sciences Ireland UC July 6 2015 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