Tenofovir Disoproxil Fumarate
For research use only.
Catalog No.S1400 Synonyms: GS-1278 Disoproxil Fumarate, Tenofovir DF
CAS No. 202138-50-9
Tenofovir Disoproxil Fumarate (GS-1278, Tenofovir DF) belongs to a class of antiretroviral drugs, it inhibits the activity of HIV reverse transcriptase by competing with the natural substrate deoxyadenosine 5’-triphosphate and, after incorporation into DNA, by DNA chain termination.
Selleck's Tenofovir Disoproxil Fumarate has been cited by 17 publications
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Human PBMCs containing indicated concentrations of Tenofovir disoproxil fumarate were inoculated with 5 ng mock-exposed or semen-exposed R5-HIV-luciferase, or 50 ng R5-HIV-luciferase as infectivity matched control. Infection rates were determined 3 days post inoculation.
Sci Transl Med, 2014, 6(262): 262ra157 . Tenofovir Disoproxil Fumarate purchased from Selleck.
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Choose Selective Reverse Transcriptase Inhibitors
|Description||Tenofovir Disoproxil Fumarate (GS-1278, Tenofovir DF) belongs to a class of antiretroviral drugs, it inhibits the activity of HIV reverse transcriptase by competing with the natural substrate deoxyadenosine 5’-triphosphate and, after incorporation into DNA, by DNA chain termination.|
Tenofovir is eliminated from systemic circulation renally through a combination of glomerular filtration and active tubular secretion. Tenofovir is not a substrate for human organic cation transporter type 1 (hOCT1) or hOCT2. Tenofovir accumulates to fivefold lower levels in MRP4-overexpressing cells, and its accumulation could be increased by an MRP inhibitor.  Tenofovir produces no significant changes in mitochondrial DNA (mtDNA) levels in human hepatoblastoma (HepG2) cells, skeletal muscle cells (SkMCs), or renal proximal tubule epithelial cells. Tenofovir elevates lactate production by less than 20% in HepG2 cells or SkMCs.  Tenofovir is efficiently phosphorylated to tenofovir diphosphate (TFV-DP) in both HepG2 cells and primary human hepatocytes. Tenofovir has a 50% effective concentration of 1.1 mM against HBV in cell-based assays, and potency is improved > 50-fold by the addition of bis-isoproxil progroups. Tenofovir has previously demonstrated full activity against lamivudine-resistant HBV in vitro and clinically.  Tenofovir inhibits the proliferation of liver-derived HepG2 cells and normal skeletal muscle cells with CC(50) values of 398 μM and 870 μM, respectively. Tenofovir shows substantially weaker effects on proliferation and viability of renal proximal tubule epithelial cells than cidofovir, a related nucleotide analog with the potential to induce renal tubular dysfunction. 
-  Ray AS, et al. Antimicrob Agents Chemother, 2006, 50(10), 3297-3304.
-  Birkus G, et al. Antimicrob Agents Chemother, 2002, 46(3), 716-723.
-  Delaney WE 4th, et al. Antimicrob Agents Chemother, 2006, 50(7), 2471-2477.
|In vitro||DMSO||100 mg/mL (157.35 mM)|
* 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.
|Synonyms||GS-1278 Disoproxil Fumarate, Tenofovir DF|
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
|Step 2: Enter the in vivo formulation ()|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
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.
1.Please make sure the liquid is clear before adding the next solvent.
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Molecular Weight Calculator
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Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03361956||Completed||Drug: JNJ-56136379|Drug: Placebo|Drug: NA (ETV or TDF)||Hepatitis B||Janssen Sciences Ireland UC||February 13 2018||Phase 2|
|NCT02985996||Completed||Drug: Truvada|Drug: Genvoya||HIV Infections||Emory University|Centers for Disease Control and Prevention||February 6 2017||Phase 1|
|NCT03043326||Recruiting||Drug: Tenofovir Disoproxil Fumarate and Emtricitabine||HIV Prevention||Asociación Civil Impacta Salud y Educación Peru|Gilead Sciences||January 23 2017||--|
|NCT01902472||Completed||--||HIV||Gilead Sciences||September 2 2013||--|
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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