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Tenofovir

Synonyms: GS-1278

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

Tenofovir Chemical Structure

Tenofovir Chemical Structure

CAS No. 147127-20-6

Purity & Quality Control

Tenofovir Related Products

Signaling Pathway

Reverse Transcriptase Signaling Pathways

Reverse Transcriptase Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human MT2 cells Function assay 5 days Antiviral activity against HIV1 3B infected in human MT2 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by XTT assay, EC50=0.013 μM 20409721
human H9 cells Function assay Antiviral activity against HIV1 clade F isolate 2338 infected in human H9 cells assessed as inhibition of viral replication, EC50=0.04 μM 21803462
C3H/3T3 cells Function assay 6 days Inhibition of murine sarcoma virus-induced transformation of mouse embryo fibroblast C3H/3T3 cells after 6 days, EC50=0.23 μM 18556209
CEM (human leukemia) cells Function assay Antiviral activity against HIV-1 (IIIB) in CEM (human leukemia) cells, EC50=1.2 μM 14584956
MT-4 cells Function assay In vitro antiviral activity against HIV-2 in MT-4 cells, EC50=1.4 μM 11327587
human bone marrow cells Cytotoxicity assay 24 h Cytotoxicity against human bone marrow cells after 24 hrs by BFU-E assay, CC50=3.5 μM 20439609
C8166 cells Function assay 4 days Antiviral activity against 100 TCID50 wild-type Human immunodeficiency virus type 2 ROD infected in C8166 cells assessed as inhibition of syncytia formation after 4 days by microscopic analysis, EC50=7.1 μM 21803462
mouse L1210 cells Cytotoxicity assay 48 h Cytostatic activity against mouse L1210 cells after 48 hrs by coulter counting analysis, IC50=11 μM 24686012
human HepG2 cells Function assay 9 days Antiviral activity against Hepatitis B virus infected human HepG2 cells after 9 days by MTT assay, IC50=12.3 μM 17888662
human HeLa cells Cytotoxicity assay 72 h Cytostatic activity against human HeLa cells after 72 hrs by coulter counting analysis, IC50=17 μM 24686012
CHO cells Cytotoxicity assay 120 h Cytotoxicity against CHO cells after 120 hrs by Cell-Titer Glo assay, CC50=21 μM 19001108
MDCK2 cells Function assay 10 μM Inhibition of human MRP3 expressed in MDCK2 cells assessed as increase in intracellular CMF fluorescence at 10 uM by CMFDA assay 17172311
human HepG2 cells Cytotoxicity assay 14 days Cytotoxicity against human HepG2 cells assessed as inhibition of cellular DNA replication after 14 days 20409721
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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
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]
In Vivo
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]
Animal Research Animal Models Macaques
Dosages 30 mg/kg
Administration Subcutaneously

Chemical Information & Solubility

Molecular Weight 287.21 Formula

C9H14N5O4P
CAS No. 147127-20-6 SDF Download Tenofovir SDF
Smiles CC(CN1C=NC2=C(N=CN=C21)N)OCP(=O)(O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 4 mg/mL ( (13.92 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 2 mg/mL

Ethanol : Insoluble


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In vivo
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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.

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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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