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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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 MUTGeY5kfGmxbjDhd5NigQ>? MUe1JIRigXN? MWfBcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDDITXYyKDOEIHnu[oVkfGWmIHnuJIh2dWGwIF3UNkBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oII\pdpV{NWmwZIXj[YQh[3m2b4DheIhq[yCnZn\lZ5Qh[W[2ZYKgOUBl[Xm|IHL5JHhVXCCjc4PhfUwhTUN3ME2wMlAyOyEQvF2= MkO1NlA1ODl5MkG=
human H9 cells MUnGeY5kfGmxbjDhd5NigQ>? MofrRY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTGlXOSClbHHk[UBHKGm|b3zheIUhOjN|ODDpcoZm[3SnZDDpckBpfW2jbjDIPUBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oII\pdoFtKHKncHzpZ4F1cW:wLDDFR|UxRTBwMESg{txO NHKwVlYzOThyM{S2Ni=>
C3H/3T3 cells M{PJUmZ2dmO2aX;uJIF{e2G7 NHP6Vo43KGSjeYO= NFTtd3BKdmirYnn0bY9vKG:oIH31dolv\SC|YYLjc41iKH[rcoXzMYlv\HWlZXSgeJJidnOob4LtZZRqd25ib3[gcY92e2ViZX3idplwKG[rYoLvZoxie3RiQ{PIM|NVOyClZXzsd{Bi\nSncjC2JIRigXNuIFXDOVA:OC5{MzFOwG0> MnfFNVg2PTZ{MEm=
CEM (human leukemia) cells MXPGeY5kfGmxbjDhd5NigQ>? NE[xcGFCdnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEBJUVZvMTCoTWlKSiliaX6gR2VOKCiqdX3hckBt\XWtZX3pZUkh[2WubIOsJGVEPTB;MT6yJO69VQ>? MlP0NVQ2QDR7NU[=
MT-4 cells M364TmZ2dmO2aX;uJIF{e2G7 M3vMWWlvKH[rdILvJIFvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JGhKXi1{IHnuJG1VNTRiY3XscJMtKEWFNUC9NU41KM7:TR?= NX71d5g2OTF|Mke1PFc>
human bone marrow cells MV\DfZRwfG:6aXPpeJkh[XO|YYm= MkDSNlQhcA>? M3rnWWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJIJwdmVibXHydo94KGOnbHzzJIFnfGW{IEK0JIhzeyCkeTDCSnUuTSCjc4PhfUwhS0N3ME2zMlUh|ryP M1nufVIxPDN7NkC5
C8166 cells M{XFcWZ2dmO2aX;uJIF{e2G7 M1PCeFQh\GG7cx?= M3\4fWFvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JFExOCCWQ1nEOVAhf2muZD30fZBmKEi3bXHuJIludXWwb3Tl[olkcWWwY4mgeolzfXNidInw[UAzKFKRRDDpcoZm[3SnZDDpckBEQDF4NjDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKHO7bnP5eIliKG[xcn3heIlwdiCjZoTldkA1KGSjeYOgZpkhdWmlcn;zZ49xcWNiYX7hcJl{cXNuIFXDOVA:Py5zIN88US=> NXrRNFFCOjF6MEO0OlI>
mouse L1210 cells M2G5[GN6fG:2b4jpZ4l1gSCjc4PhfS=> M1u3[VQ5KGh? NH;NTGZEgXSxc4TheIlkKGGldHn2bZR6KGGpYXnud5QhdW:3c3WgUFEzOTBiY3XscJMh[W[2ZYKgOFghcHK|IHL5JINwfWy2ZYKgZ492dnSrbnegZY5idHm|aYOsJGlEPTB;MUGg{txO MWqyOFY5PjBzMh?=
human HepG2 cells M3LtXGZ2dmO2aX;uJIF{e2G7 NGPX[m06KGSjeYO= NGrDcoJCdnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEBJ\XCjdHn0bZMhSiC4aYL1d{Bqdm[nY4Tl[EBpfW2jbjDI[ZBIOiClZXzsd{Bi\nSncjC5JIRigXNiYomgUXRVKGG|c3H5MEBKSzVyPUGyMlMh|ryP MmHmNVc5QDh4NkK=
human HeLa cells NFjMU25EgXSxdH;4bYNqfHliYYPzZZk> NFvtNnA4OiCq MkmxR5l1d3O2YYTpZ{Bi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjlUIEh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IHPveYx1\XJiY3;1cpRqdmdiYX7hcJl{cXNuIFnDOVA:OTdizszN NI\iXI0zPDZ6NkCxNi=>
CHO cells NYnpV25VS3m2b4TvfIlkcXS7IHHzd4F6 NGK0UIMyOjBiaB?= NWfJZ4Q4S3m2b4TvfIlkcXS7IHHnZYlve3RiQ1jPJINmdGy|IHHmeIVzKDF{MDDodpMh[nliQ3XscE1VcXSncjDHcI8h[XO|YYmsJGNEPTB;MkGg{txO NIT6VHUyQTByMUGwPC=>
MDCK2 cells M3zNbmZ2dmO2aX;uJIF{e2G7 MonsNVAh|ryP NVfRUmNCUW6qaXLpeIlwdiCxZjDoeY1idiCPUmCzJIV5eHKnc4Pl[EBqdiCPRFPLNkBk\WyuczDhd5Nme3OnZDDhd{BqdmO{ZXHz[UBqdiCrboTyZYNmdGy3bHHyJGNOTiCobIXvdoV{[2WwY3WgZZQhOTBidV2gZpkhS02IRFGgZZN{[Xl? NUnndYVFOTdzN{KzNVE>
human HepG2 cells M1X1cWN6fG:2b4jpZ4l1gSCjc4PhfS=> NVq4eFh[OTRiZHH5dy=> MomyR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTIVxTzJiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBk\WyudXzhdkBFVkFicnXwcIlk[XSrb36gZYZ1\XJiMUSg[IF6ew>? NFn1dWczODRyOUeyNS=>

... 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 individually and in order:
30% propylene glycol, 5% Tween 80, 65% D5W
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
Synonyms GS-1278

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03032536 Recruiting Hepatitis B|Chronic Hepatitis B|Viral Hepatitis B Alios Biopharma Inc. January 31, 2017 Phase 1
NCT03048422 Not yet recruiting HIV Infections National Institute of Allergy and Infectious Diseases (NIAID) April 30, 2017 Phase 3
NCT00524173 Recruiting Hepatitis B National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)|National Institutes of Health Clinical Center (CC) August 29, 2007 Phase 2
NCT03043326 Recruiting HIV Prevention Asociación Civil Impacta Salud y Educación, Peru|Gilead Sciences January 23, 2017 --
NCT02454764 Not yet recruiting HBV Institute of Liver and Biliary Sciences, India May 2017 --
NCT02937779 Not yet recruiting Hepatitis B Chronic Infection|Pregnancy French National Institute for Health and Medical Research-French National Agency for Research on AIDS and Viral Hepatitis (Inserm-ANRS) April 2017 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