Tenofovir

For research use only.

Catalog No.S1401 Synonyms: GS-1278

20 publications

Tenofovir  Chemical Structure

CAS No. 147127-20-6

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

Selleck's Tenofovir has been cited by 20 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 Mlm3SpVv[3Srb36gZZN{[Xl? MYC1JIRigXN? NXTVZVlGSW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUEmYMTCzRkBqdm[nY4Tl[EBqdiCqdX3hckBOXDJiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kB3cXK3cz3pcoR2[2WmIHP5eI9x[XSqaXOg[YZn\WO2IHHmeIVzKDViZHH5d{BjgSC[VGSgZZN{[XluIFXDOVA:OC5yMUOg{txO M1\ZO|IxPDB7N{Kx
human H9 cells NGSxc2pHfW6ldHnvckBie3OjeR?= NUnhNXo6SW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUEmYMTDjcIFl\SCIIHnzc4xifGViMkOzPEBqdm[nY4Tl[EBqdiCqdX3hckBJQSClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJJZqemGuIILldIxq[2G2aX;uMEBGSzVyPUCuNFQh|ryP M2HC[lIyQDB|NE[y
C3H/3T3 cells MnjjSpVv[3Srb36gZZN{[Xl? NWjLUnJNPiCmYYnz M1jj[WlvcGmkaYTpc44hd2ZibYXybY5mKHOjcnPvcYEhfmm{dYOtbY5lfWOnZDD0doFve2[xcn3heIlwdiCxZjDtc5V{\SCnbXLyfY8h\mmkcn;icIF{fCCFM1ivN3Q{KGOnbHzzJIFnfGW{IE[g[IF6eyxiRVO1NF0xNjJ|IN88US=> NEPzUlMyQDV3NkKwPS=>
CEM (human leukemia) cells NYfIc5ZDTnWwY4Tpc44h[XO|YYm= NV7oU2J3SW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUEmYLUGgLGlKUUJrIHnuJGNGVSBqaIXtZY4hdGW3a3XtbYEqKGOnbHzzMEBGSzVyPUGuNkDPxE1? MlzuNVQ2QDR7NU[=
MT-4 cells MULGeY5kfGmxbjDhd5NigQ>? Mne4TY4hfmm2cn:gZY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTGlXNTJiaX6gUXQuPCClZXzsd{whTUN3ME2xMlQh|ryP Ml7wNVE{Ojd3OEe=
human bone marrow cells M1rkTmN6fG:2b4jpZ4l1gSCjc4PhfS=> M4K3N|I1KGh? NVL5RXBKS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4h[m:wZTDtZZJzd3diY3XscJMh[W[2ZYKgNlQhcHK|IHL5JGJHXS2HIHHzd4F6NCCFQ{WwQVMvPSEQvF2= MWCyNFQ{QTZyOR?=
C8166 cells M2LyOWZ2dmO2aX;uJIF{e2G7 NU[wcopwPCCmYYnz NHHN[2FCdnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEAyODBiVFPJSFUxKHerbHSteJlx\SCKdX3hckBqdW23bn;k[YZq[2mnbnP5JJZqenW|IIT5dIUhOiCUT1SgbY5n\WO2ZXSgbY4hSzhzNk[gZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iC|eX7jfZRq[SCob4LtZZRqd25iYX\0[ZIhPCCmYYnzJIJ6KG2rY4Lvd4NweGmlIHHuZYx6e2m|LDDFR|UxRTdwMTFOwG0> MXKyNVgxOzR4Mh?=
mouse L1210 cells M4HXSGN6fG:2b4jpZ4l1gSCjc4PhfS=> NGnLZmQ1QCCq M2\6dWN6fG:|dHH0bYMh[WO2aY\peJkh[WejaX7zeEBud3W|ZTDMNVIyOCClZXzsd{Bi\nSncjC0PEBpenNiYomgZ492dHSncjDjc5VvfGmwZzDhcoFtgXOrczygTWM2OD1zMTFOwG0> MWeyOFY5PjBzMh?=
human HepG2 cells MVLGeY5kfGmxbjDhd5NigQ>? MWm5JIRigXN? MkDtRY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTIVx[XSrdHnzJGIhfmm{dYOgbY5n\WO2ZXSgbJVu[W5iSHXwS|Ih[2WubIOgZYZ1\XJiOTDkZZl{KGK7IF3UWEBie3OjeTygTWM2OD1zMj6zJO69VQ>? NWjVRoo1OTd6OEi2OlI>
human HeLa cells MoDkR5l1d3SxeHnjbZR6KGG|c3H5 NWPrXFZYPzJiaB?= M4rrXWN6fG:|dHH0bYMh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDI[WxiKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDjc5VtfGW{IHPveY51cW6pIHHuZYx6e2m|LDDJR|UxRTF5IN88US=> M3\JS|I1Pjh4MEGy
CHO cells M3TJRWN6fG:2b4jpZ4l1gSCjc4PhfS=> NViyc4R4OTJyIHi= NFT1cHlEgXSxdH;4bYNqfHliYXfhbY5{fCCFSF:gZ4VtdHNiYX\0[ZIhOTJyIHjyd{BjgSCFZXzsMXRqfGW{IFfsc{Bie3OjeTygR2M2OD1{MTFOwG0> MWKxPVAxOTFyOB?=
MDCK2 cells MmTGSpVv[3Srb36gZZN{[Xl? MofXNVAh|ryP NXXGRZF4UW6qaXLpeIlwdiCxZjDoeY1idiCPUmCzJIV5eHKnc4Pl[EBqdiCPRFPLNkBk\WyuczDhd5Nme3OnZDDhd{BqdmO{ZXHz[UBqdiCrboTyZYNmdGy3bHHyJGNOTiCobIXvdoV{[2WwY3WgZZQhOTBidV2gZpkhS02IRFGgZZN{[Xl? MYKxO|E4OjNzMR?=
human HepG2 cells NXTZOGFLS3m2b4TvfIlkcXS7IHHzd4F6 M4HESFE1KGSjeYO= MWrDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDI[ZBIOiClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJINmdGy3bHHyJGRPSSC{ZYDsbYNifGmxbjDh[pRmeiBzNDDkZZl{ M2XXdVIxPDB7N{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
  • 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
Smiles CC(CN1C=NC2=C(N=CN=C21)N)OCP(=O)(O)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04782180 Not yet recruiting Drug: Descovy 200Mg 25Mg Tablet|Behavioral: PrEP Hiv|Substance Use Disorders University of Miami October 1 2021 Phase 4
NCT04195776 Recruiting Drug: Tenofovir Douche HIV/AIDS|HIV Prevention Johns Hopkins University|National Institute of Allergy and Infectious Diseases (NIAID)|CONRAD June 1 2021 Phase 1
NCT04867798 Not yet recruiting Drug: Lamivudine-Tenofovir 300 Mg-300 Mg Oral Tablet HIV|Sexually Transmitted Infections|PrEP|Transgender Men Makerere University|Massachusetts General Hospital June 2021 --

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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.

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Reverse Transcriptase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID