Tenofovir

Catalog No.S1401 Synonyms: GS-1278

For research use only.

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

Tenofovir  Chemical Structure

CAS No. 147127-20-6

Selleck's Tenofovir has been cited by 22 publications

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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.
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 NYfzZ3U4TnWwY4Tpc44h[XO|YYm= NIS4WWo2KGSjeYO= MWrBcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDDITXYyKDOEIHnu[oVkfGWmIHnuJIh2dWGwIF3UNkBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oII\pdpV{NWmwZIXj[YQh[3m2b4DheIhq[yCnZn\lZ5Qh[W[2ZYKgOUBl[Xm|IHL5JHhVXCCjc4PhfUwhTUN3ME2wMlAyOyEQvF2= MUGyNFQxQTd{MR?=
human H9 cells NWXwSWc4TnWwY4Tpc44h[XO|YYm= NYfZR|BxSW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUEmYMTDjcIFl\SCIIHnzc4xifGViMkOzPEBqdm[nY4Tl[EBqdiCqdX3hckBJQSClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJJZqemGuIILldIxq[2G2aX;uMEBGSzVyPUCuNFQh|ryP MV6yNVgxOzR4Mh?=
C3H/3T3 cells Ml7ySpVv[3Srb36gZZN{[Xl? NUSzWYxmPiCmYYnz M4PKOWlvcGmkaYTpc44hd2ZibYXybY5mKHOjcnPvcYEhfmm{dYOtbY5lfWOnZDD0doFve2[xcn3heIlwdiCxZjDtc5V{\SCnbXLyfY8h\mmkcn;icIF{fCCFM1ivN3Q{KGOnbHzzJIFnfGW{IE[g[IF6eyxiRVO1NF0xNjJ|IN88US=> MV2xPFU2PjJyOR?=
CEM (human leukemia) cells MmjZSpVv[3Srb36gZZN{[Xl? MnXkRY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTGlXNTFiKFnJTWIqKGmwIFPFUUApcHWvYX6gcIV2c2WvaXGpJINmdGy|LDDFR|UxRTFwMjFOwG0> M1W3VVE1PTh2OUW2
MT-4 cells MlzqSpVv[3Srb36gZZN{[Xl? NHvVN2tKdiC4aYTyc{BidnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEBJUVZvMjDpckBOXC12IHPlcIx{NCCHQ{WwQVEvPCEQvF2= MlrvNVE{Ojd3OEe=
human bone marrow cells MVvDfZRwfG:6aXPpeJkh[XO|YYm= M3P3OlI1KGh? NHHwbnBEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBjd26nIH3hdpJwfyClZXzsd{Bi\nSncjCyOEBpenNiYomgRmZWNUViYYPzZZktKEOFNUC9N{42KM7:TR?= NHvyN2UzODR|OU[wPS=>
C8166 cells MXTGeY5kfGmxbjDhd5NigQ>? NHyyfVA1KGSjeYO= Mn7wRY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgNVAxKFSFSVS1NEB4cWymLYT5dIUhUHWvYX6gbY1ufW6xZHXmbYNq\W6leTD2bZJ2eyC2eYDlJFIhWk:GIHnu[oVkfGWmIHnuJGM5OTZ4IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4Yhe3mwY4n0bYEh\m:{bXH0bY9vKGGodHXyJFQh\GG7czDifUBucWO{b4Pjc5Bq[yCjbnHsfZNqeyxiRVO1NF04NjFizszN NGDHfG4zOThyM{S2Ni=>
mouse L1210 cells NWTVbYJzS3m2b4TvfIlkcXS7IHHzd4F6 M1rHV|Q5KGh? MUjDfZRwe3SjdHnjJIFkfGm4aYT5JIFo[Wmwc4SgcY92e2ViTEGyNVAh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IHPveYx1\XJiY3;1cpRqdmdiYX7hcJl{cXNuIFnDOVA:OTFizszN NWHabmlWOjR4OE[wNVI>
human HepG2 cells M4r0XGZ2dmO2aX;uJIF{e2G7 MUe5JIRigXN? M{nxXGFvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JGhmeGG2aYTpd{BDKH[rcoXzJIlv\mWldHXkJIh2dWGwIFjldGczKGOnbHzzJIFnfGW{IEmg[IF6eyCkeTDNWHQh[XO|YYmsJGlEPTB;MUKuN{DPxE1? MUexO|g5QDZ4Mh?=
human HeLa cells M1;5T2N6fG:2b4jpZ4l1gSCjc4PhfS=> MYG3NkBp NF7qXpVEgXSxc4TheIlkKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gTIVN[SClZXzsd{Bi\nSncjC3NkBpenNiYomgZ492dHSncjDjc5VvfGmwZzDhcoFtgXOrczygTWM2OD1zNzFOwG0> NXHhc5hzOjR4OE[wNVI>
CHO cells NIHKbGZEgXSxdH;4bYNqfHliYYPzZZk> NHfZbIMyOjBiaB?= NYnxR4FXS3m2b4TvfIlkcXS7IHHnZYlve3RiQ1jPJINmdGy|IHHmeIVzKDF{MDDodpMh[nliQ3XscE1VcXSncjDHcI8h[XO|YYmsJGNEPTB;MkGg{txO NIH1THgyQTByMUGwPC=>
MDCK2 cells M2\zO2Z2dmO2aX;uJIF{e2G7 NUHCSJlbOTBizszN MYfJcohq[mm2aX;uJI9nKGi3bXHuJG1TWDNiZYjwdoV{e2WmIHnuJG1FS0t{IHPlcIx{KGG|c3Xzd4VlKGG|IHnuZ5Jm[XOnIHnuJIlvfHKjY3XscJVt[XJiQ13GJIZtfW:{ZYPj[Y5k\SCjdDCxNEB2VSCkeTDDUWZFSSCjc4PhfS=> MoLhNVcyPzJ|MUG=
human HepG2 cells M{PoWGN6fG:2b4jpZ4l1gSCjc4PhfS=> NYrDNm5bOTRiZHH5dy=> M3XneWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhmeEd{IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4Yh[2WubIXsZZIhTE6DIILldIxq[2G2aX;uJIFnfGW{IEG0JIRigXN? NFG0[XAzODRyOUeyNS=>
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 (from reference)

Animal Research:[1]
  • Animal Models: Macaques
  • Dosages: 30 mg/kg
  • Administration: Subcutaneously

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 287.21
Formula

C9H14N5O4P

CAS No. 147127-20-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(CN1C=NC2=C(N=CN=C21)N)OCP(=O)(O)O

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05140954 Not yet recruiting Drug: co-formulated 25mg TAF/ 200mg FTC HIV Infections University of Washington|Kenya Medical Research Institute|University of Colorado Denver|Gilead Sciences September 2022 Phase 2|Phase 3
NCT05057858 Enrolling by invitation Drug: co-formulated 300 mg TDF/ 200mg FTC HIV Infections University of Washington|University of Colorado Denver|Kenya Medical Research Institute|National Institute of Allergy and Infectious Diseases (NIAID) April 25 2022 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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