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.

Size Price Stock Quantity  
10mM (1mL in DMSO) USD 110 In stock
USD 97 In stock
USD 270 In stock
USD 570 In stock
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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 MWDGeY5kfGmxbjDhd5NigQ>? NX7EUpRmPSCmYYnz MULBcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDDITXYyKDOEIHnu[oVkfGWmIHnuJIh2dWGwIF3UNkBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oII\pdpV{NWmwZIXj[YQh[3m2b4DheIhq[yCnZn\lZ5Qh[W[2ZYKgOUBl[Xm|IHL5JHhVXCCjc4PhfUwhTUN3ME2wMlAyOyEQvF2= MljINlA1ODl5MkG=
human H9 cells MlX2SpVv[3Srb36gZZN{[Xl? Mo[2RY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTGlXOSClbHHk[UBHKGm|b3zheIUhOjN|ODDpcoZm[3SnZDDpckBpfW2jbjDIPUBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oII\pdoFtKHKncHzpZ4F1cW:wLDDFR|UxRTBwMESg{txO NHPac|UzOThyM{S2Ni=>
C3H/3T3 cells NIXt[|FHfW6ldHnvckBie3OjeR?= NGTURYk3KGSjeYO= MnzVTY5pcWKrdHnvckBw\iCvdYLpcoUhe2G{Y3;tZUB3cXK3cz3pcoR2[2WmIITyZY5{\m:{bXH0bY9vKG:oIH3veZNmKGWvYoL5c{BncWK{b3LsZZN1KEN|SD:zWFMh[2WubIOgZYZ1\XJiNjDkZZl{NCCHQ{WwQVAvOjNizszN NVrON3ZxOTh3NU[yNFk>
CEM (human leukemia) cells MXjGeY5kfGmxbjDhd5NigQ>? MmDsRY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTGlXNTFiKFnJTWIqKGmwIFPFUUApcHWvYX6gcIV2c2WvaXGpJINmdGy|LDDFR|UxRTFwMjFOwG0> MX:xOFU5PDl3Nh?=
MT-4 cells M2nCPGZ2dmO2aX;uJIF{e2G7 NVK4[3hSUW5idnn0do8h[W62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUEmYLUKgbY4hVVRvNDDj[YxteyxiRVO1NF0yNjRizszN NH6zRYgyOTN{N{W4Oy=>
human bone marrow cells NEC5N45EgXSxdH;4bYNqfHliYYPzZZk> M2fpTFI1KGh? NGj6NWdEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBjd26nIH3hdpJwfyClZXzsd{Bi\nSncjCyOEBpenNiYomgRmZWNUViYYPzZZktKEOFNUC9N{42KM7:TR?= M4nu[VIxPDN7NkC5
C8166 cells NHe0WHhHfW6ldHnvckBie3OjeR?= M2jQS|Qh\GG7cx?= MUTBcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDCxNFAhXEOLREWwJJdqdGRvdInw[UBJfW2jbjDpcY12dm:mZX\pZ4lmdmO7II\pdpV{KHS7cHWgNkBTV0RiaX7m[YN1\WRiaX6gR|gyPjZiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kB{gW6leYTpZUBnd3KvYYTpc44h[W[2ZYKgOEBl[Xm|IHL5JI1q[3Kxc3PvdIlkKGGwYXz5d4l{NCCHQ{WwQVcvOSEQvF2= MmnENlE5ODN2NkK=
mouse L1210 cells NG\RTGREgXSxdH;4bYNqfHliYYPzZZk> MmL0OFghcA>? NYrkd|BrS3m2b4P0ZZRq[yCjY4Tpeol1gSCjZ3HpcpN1KG2xdYPlJGwyOjFyIHPlcIx{KGGodHXyJFQ5KGi{czDifUBkd3WudHXyJINwfW62aX7nJIFv[Wy7c3nzMEBKSzVyPUGxJO69VQ>? NXXoV3J[OjR4OE[wNVI>
human HepG2 cells M4HvdmZ2dmO2aX;uJIF{e2G7 NX24UHRzQSCmYYnz MoPXRY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTIVx[XSrdHnzJGIhfmm{dYOgbY5n\WO2ZXSgbJVu[W5iSHXwS|Ih[2WubIOgZYZ1\XJiOTDkZZl{KGK7IF3UWEBie3OjeTygTWM2OD1zMj6zJO69VQ>? NGToPXAyPzh6OE[2Ni=>
human HeLa cells MYfDfZRwfG:6aXPpeJkh[XO|YYm= M3\QWFczKGh? MoLER5l1d3O2YYTpZ{Bi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjlUIEh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IHPveYx1\XJiY3;1cpRqdmdiYX7hcJl{cXNuIFnDOVA:OTdizszN MkTQNlQ3QDZyMUK=
CHO cells NFvVflhEgXSxdH;4bYNqfHliYYPzZZk> NH7zepYyOjBiaB?= NED4V5FEgXSxdH;4bYNqfHliYXfhbY5{fCCFSF:gZ4VtdHNiYX\0[ZIhOTJyIHjyd{BjgSCFZXzsMXRqfGW{IFfsc{Bie3OjeTygR2M2OD1{MTFOwG0> MUKxPVAxOTFyOB?=
MDCK2 cells NGXNOo1HfW6ldHnvckBie3OjeR?= MX[xNEDPxE1? NELTWXVKdmirYnn0bY9vKG:oIHj1cYFvKE2UUEOg[ZhxemW|c3XkJIlvKE2GQ1uyJINmdGy|IHHzd4V{e2WmIHHzJIlv[3KnYYPlJIlvKGmwdILhZ4VtdHWuYYKgR21HKG[udX;y[ZNk\W6lZTDheEAyOCC3TTDifUBEVU[GQTDhd5NigQ>? NIPmfocyPzF5MkOxNS=>
human HepG2 cells MmnoR5l1d3SxeHnjbZR6KGG|c3H5 Mn\HNVQh\GG7cx?= NUDPN5dQS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUGWyR{KgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iClZXzseYxieiCGTlGgdoVxdGmlYYTpc44h[W[2ZYKgNVQh\GG7cx?= MlXCNlA1ODl5MkG=

... 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

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04195776 Not yet 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
NCT03789968 Completed Drug: bictegravir/emtricitabine/tenofovir alafenamide HIV/AIDS Thomas Jefferson University|University of Maryland College Park|Indiana University Health|The Brooklyn Hospital Center|University of Illinois at Chicago|Nova Southeastern University|University of California San Francisco September 1 2019 --
NCT02722343 Completed Drug: Tenofovir intravaginal ring|Drug: Truvada HIV CONRAD|Eastern Virginia Medical School|University of North Carolina|Agility Clinical Inc. April 2016 Phase 1
NCT02588287 Active not recruiting Other: Blood draws for tenofovir PK renal function Hepatitis C and HIV Coinfection University of Colorado Denver November 2015 Not Applicable
NCT02280109 Completed Drug: Tenofovir Gel|Drug: Tenofovir Film Healthy|HIV CONRAD|National Institute of Allergy and Infectious Diseases (NIAID) November 2014 Early Phase 1

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Reverse Transcriptase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID