Catalog No.S1401 Synonyms: GS-1278
Molecular Weight(MW): 287.21
Tenofovir blocks reverse transcriptase and hepatitis B virus infections.
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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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|Description||Tenofovir blocks reverse transcriptase and hepatitis B virus infections.|
|Features||Tenofovir disoproxil fumarate is the prodrug form of tenofovir.|
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).  Tenofovir is uniquely active against multinucleoside-resistant HIV expressing the Q151M mutation, but shows reduced susceptibility to the T69S insertion mutations.  Tenofovir inhibits hepatitis B virus (HBV) activity in HepG2 2.2.15, HepAD38 and HepAD79 cells.  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. 
|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. |
-  Witvrouw M, et al. Antivir Ther, 2004, 9(1), 57-65.
-  Miller MD, et al. Nucleosides Nucleotides Nucleic Acids, 2001, 20(4-7), 1025-1028.
-  Ying C, et al. J Viral Hepat, 2000, 7(2), 161-165.
|In vitro||DMSO||4 mg/mL warmed (13.92 mM)|
|Water||2 mg/mL (6.96 mM)|
|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.
* 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.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03251144||Recruiting||HIV/AIDS|Antiviral Toxicity|Antiviral Drug Adverse Reaction|Mitochondrial Alteration||University of California Los Angeles|Gilead Sciences||September 8 2018||Phase 1|Phase 2|
|NCT03126370||Recruiting||Hepatitis C|HIV Coinfection||University of Colorado Denver||January 8 2018||Phase 4|
|NCT03067285||Recruiting||HIV Infections||Fundacion SEIMC-GESIDA||September 8 2017||Phase 4|
|NCT03060785||Completed||HIV Prevention||Johns Hopkins University||March 8 2016||Phase 1|
|NCT03425994||Recruiting||Chronic Hepatitis B in HIV Patient|Kidney Injury|Bone Diseases||National Taiwan University Hospital|National Taiwan University Hospital Hsin-Chu Branch|National Taiwan University Hospital Yun-Lin Branch|Far Eastern Memorial Hospital|Taoyuan General Hospital|Mackay Memorial Hospital|Chung Shan Medical University|Taichung Veterans General Hospital|National Cheng-Kung University Hospital|Changhua Christian Hospital|Chi Mei Medical Hospital|Kaohsiung Veterans General Hospital.|Kaohsiung Medical University Chung-Ho Memorial Hospital|Chang Gung Memorial Hospital|E-DA Hospital|Lotung Poh-Ai Hospital||February 6 2018||--|
|NCT02431247||Active not recruiting||Immunodeficiency Virus Type 1 Human||Janssen Sciences Ireland UC||July 6 2015||Phase 3|
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