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 5 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 NF7PZ5JHfW6ldHnvckBie3OjeR?= MnyxOUBl[Xm| MULBcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDDITXYyKDOEIHnu[oVkfGWmIHnuJIh2dWGwIF3UNkBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oII\pdpV{NWmwZIXj[YQh[3m2b4DheIhq[yCnZn\lZ5Qh[W[2ZYKgOUBl[Xm|IHL5JHhVXCCjc4PhfUwhTUN3ME2wMlAyOyEQvF2= NFW2Z2czODRyOUeyNS=>
human H9 cells M3XQVmZ2dmO2aX;uJIF{e2G7 NGrIbVFCdnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEBJUVZzIHPsZYRmKEZiaYPvcIF1\SB{M{O4JIlv\mWldHXkJIlvKGi3bXHuJGg6KGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[geolz[WxicnXwcIlk[XSrb36sJGVEPTB;MD6wOEDPxE1? NGrLS5MzOThyM{S2Ni=>
C3H/3T3 cells M3HGRmZ2dmO2aX;uJIF{e2G7 NEfnN4s3KGSjeYO= NXLm[FlWUW6qaXLpeIlwdiCxZjDteZJqdmVic3HyZ49u[SC4aYL1d{1qdmS3Y3XkJJRz[W6|Zn;ycYF1cW:wIH;mJI1wfXOnIHXtZpJ6dyCoaXLyc4Jt[XO2IFOzTE8{XDNiY3XscJMh[W[2ZYKgOkBl[Xm|LDDFR|UxRTBwMkOg{txO MoPjNVg2PTZ{MEm=
CEM (human leukemia) cells NUXuWWxETnWwY4Tpc44h[XO|YYm= MWTBcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDDITXYuOSBqSVnJRkkhcW5iQ1XNJEhpfW2jbjDs[ZVs\W2rYTmgZ4VtdHNuIFXDOVA:OS5{IN88US=> NGnPcmQyPDV6NEm1Oi=>
MT-4 cells MU\GeY5kfGmxbjDhd5NigQ>? MoW2TY4hfmm2cn:gZY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTGlXNTJiaX6gUXQuPCClZXzsd{whTUN3ME2xMlQh|ryP MYKxNVMzPzV6Nx?=
human bone marrow cells NVfLfIJCS3m2b4TvfIlkcXS7IHHzd4F6 NGXGRlEzPCCq NYnUOnNuS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4h[m:wZTDtZZJzd3diY3XscJMh[W[2ZYKgNlQhcHK|IHL5JGJHXS2HIHHzd4F6NCCFQ{WwQVMvPSEQvF2= MojuNlA1Ozl4MEm=
C8166 cells M4TjVGZ2dmO2aX;uJIF{e2G7 MmjFOEBl[Xm| MYjBcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDCxNFAhXEOLREWwJJdqdGRvdInw[UBJfW2jbjDpcY12dm:mZX\pZ4lmdmO7II\pdpV{KHS7cHWgNkBTV0RiaX7m[YN1\WRiaX6gR|gyPjZiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kB{gW6leYTpZUBnd3KvYYTpc44h[W[2ZYKgOEBl[Xm|IHL5JI1q[3Kxc3PvdIlkKGGwYXz5d4l{NCCHQ{WwQVcvOSEQvF2= NWHNSld1OjF6MEO0OlI>
mouse L1210 cells M3zGRmN6fG:2b4jpZ4l1gSCjc4PhfS=> MoDQOFghcA>? MknzR5l1d3O2YYTpZ{Bi[3Srdnn0fUBi\2GrboP0JI1wfXOnIFyxNlExKGOnbHzzJIFnfGW{IES4JIhzeyCkeTDjc5VtfGW{IHPveY51cW6pIHHuZYx6e2m|LDDJR|UxRTFzIN88US=> MnXsNlQ3QDZyMUK=
human HepG2 cells NEHlVGVHfW6ldHnvckBie3OjeR?= MlzqPUBl[Xm| NEDqXldCdnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEBJ\XCjdHn0bZMhSiC4aYL1d{Bqdm[nY4Tl[EBpfW2jbjDI[ZBIOiClZXzsd{Bi\nSncjC5JIRigXNiYomgUXRVKGG|c3H5MEBKSzVyPUGyMlMh|ryP MXOxO|g5QDZ4Mh?=
human HeLa cells NYHZO3B7S3m2b4TvfIlkcXS7IHHzd4F6 MX23NkBp NF7mXpNEgXSxc4TheIlkKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gTIVN[SClZXzsd{Bi\nSncjC3NkBpenNiYomgZ492dHSncjDjc5VvfGmwZzDhcoFtgXOrczygTWM2OD1zNzFOwG0> MUSyOFY5PjBzMh?=
CHO cells MlLBR5l1d3SxeHnjbZR6KGG|c3H5 M4fmPVEzOCCq MmLRR5l1d3SxeHnjbZR6KGGpYXnud5QhS0iRIHPlcIx{KGGodHXyJFEzOCCqcoOgZpkhS2WubD3UbZRmeiCJbH:gZZN{[XluIFPDOVA:OjFizszN NGr0UGsyQTByMUGwPC=>
MDCK2 cells NEfQSVJHfW6ldHnvckBie3OjeR?= M{\jXlExKM7:TR?= MnO2TY5pcWKrdHnvckBw\iCqdX3hckBOWlB|IHX4dJJme3OnZDDpckBOTEONMjDj[YxteyCjc4Pld5Nm\CCjczDpcoNz\WG|ZTDpckBqdnS{YXPlcIx2dGG{IFPNSkBndHWxcnXzZ4Vv[2ViYYSgNVAhfU1iYomgR21HTEFiYYPzZZk> NHHJPZMyPzF5MkOxNS=>
human HepG2 cells MVzDfZRwfG:6aXPpeJkh[XO|YYm= M2LzeFE1KGSjeYO= NWTJR45DS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUGWyR{KgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iClZXzseYxieiCGTlGgdoVxdGmlYYTpc44h[W[2ZYKgNVQh\GG7cx?= MmS1NlA1ODl5MkG=

... 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]
+ Expand
  • 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
NCT03789968 Not yet recruiting HIV/AIDS Thomas Jefferson University|University of Maryland|Indiana University Health|The Brooklyn Hospital Center|University of Illinois at Chicago|Nova Southeastern University|University of California San Francisco March 1 2019 --
NCT03798119 Not yet recruiting Hepatitis B|Fibrosis and Cirrhosis of Liver Kaohsiung Medical University Chung-Ho Memorial Hospital March 1 2019 Phase 4
NCT03804372 Not yet recruiting Large-B-cell Diffuse Lymphoma|Chronic Lymphoid Leukemia Gruppo Italiano Malattie EMatologiche dell''Adulto March 2019 Phase 2
NCT03789968 Not yet recruiting HIV/AIDS Thomas Jefferson University|University of Maryland|Indiana University Health|The Brooklyn Hospital Center|University of Illinois at Chicago|Nova Southeastern University|University of California San Francisco March 1 2019 --
NCT03804372 Not yet recruiting Large-B-cell Diffuse Lymphoma|Chronic Lymphoid Leukemia Gruppo Italiano Malattie EMatologiche dell''Adulto March 2019 Phase 2
NCT03798119 Not yet recruiting Hepatitis B|Fibrosis and Cirrhosis of Liver Kaohsiung Medical University Chung-Ho Memorial Hospital March 1 2019 Phase 4

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Reverse Transcriptase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID