Home Microbiology Reverse Transcriptase inhibitor - HIV inhibitor Tenofovir Disoproxil Fumarate For research use only.

Tenofovir Disoproxil Fumarate

Synonyms: GS 1278, Tenofovir DF

Tenofovir Disoproxil Fumarate 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 Disoproxil Fumarate Chemical Structure

Tenofovir Disoproxil Fumarate Chemical Structure

CAS: 202138-50-9

Selleck's Tenofovir Disoproxil Fumarate has been cited by 25 Publications

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Purity & Quality Control

Batch: Purity: 99.94%
99.94

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MT2 Function assay 5 days Inhibition of virus-induced cytopathic effect in wild type HIV 3a infected MT2 cells after 5 days, EC50=0.015μM 17562366
HepG2 Cytotoxicity assay 9 days Cytotoxicity against human HepG2 cells after 9 days by MTT assay, IC50=2.31μM 17888662
HepG2 Antiviral assay 9 days Antiviral activity against Hepatitis B virus infected human HepG2 cells after 9 days by MTT assay, IC50=5.1μM 17888662
MT-2 Antiviral assay Antiviral activity against HIV1 3B infected in human MT-2 cells by two fold dilution method in presence of 10% FBS, EC50=0.0068μM 19104010
MT2 Antiviral assay Antiviral activity against HIV1 infected in human MT2 cells assessed as inhibition of viral replication, IC50=0.54μM 19596885
HeLa P4/R5 Antiviral assay Antiviral activity against HIV1 infected in human HeLa P4/R5 cells assessed as inhibition of viral replication, IC50=4.7μM 19596885
HeLa P4/R5 Antiviral assay Antiviral activity against HIV1 harboring reverse transcriptase K65R mutant infected in human HeLa P4/R5 cells assessed as inhibition of viral replication, IC50=11.4μM 19596885
human bone marrow cells Cytotoxicity assay 24 hrs Cytotoxicity against human bone marrow cells after 24 hrs by BFU-E assay, CC50=0.9μM 20439609
human bone marrow cells Cytotoxicity assay 24 hrs Cytotoxicity against human bone marrow cells after 24 hrs by GM-CFU assay, CC50=1.9μM 20439609
HeLa-T4 Antiviral assay 48 hrs Antiviral activity against single-round HIV1 NLX.Lux-R harboring inactivating mutations in env, vpr and carries firefly luciferase gene in place of nef infected in human HeLa-T4 cells assessed as luciferase activity after 48 hrs by exogenous RT assay, EC50=0.0029μM 21060108
HeLa-T4 Antiviral assay 48 hrs Antiviral activity against single-round HIV1 NLX.Lux-R harboring inactivating mutations in env, vpr and carries firefly luciferase gene in place of nef infected in human HeLa-T4 cells assessed as luciferase activity after 48 hrs by exogenous RT assay, EC95=0.037μM 21060108
HeLaT4 Antiviral assay 24 hrs Antiviral activity against single-round HIV1 NLX.Lux-R harboring inactivating mutations in env, vpr and carries firefly luciferase gene in place of nef assessed as level of infection using human HeLaT4 cells pretreated for 24 hrs followed by exposed to vi, EC50=0.12μM 21060108
HeLaT4 Antiviral assay Antiviral activity against single-round HIV1 NLX.Lux-R harboring inactivating mutations in env, vpr and carries firefly luciferase gene in place of nef assessed as level of 2 mins magnetic nanopartials-medated infection in human HeLaT4 cells treated for 1, EC99.6=0.95μM 21060108
HeLaT4 Cytotoxicity assay Cytotoxicity against human HeLaT4 cells by WST-1 assay, CC50=34μM 21060108
HeLaT4 Function assay 24 hrs Drug uptake in human HeLaT4 cells assessed as compound persist measured after 3 times washout at 100 time EC95 for HIV1 for 24 hrs 21060108
HeLaT4 Antiviral assay 24 hrs Antiviral activity against single-round HIV1 NLX.Lux-R harboring inactivating mutations in env, vpr and carries firefly luciferase gene in place of nef assessed as level of infection using human HeLaT4 cells pretreated at 100 time EC95 for 24 hrs followed 21060108
PBMC Antiviral assay 7 days Antiviral activity against HIV1 infected in human PBMC assessed as inhibition of viral replication by measuring reverse transcriptase activity in cell supernatant preincubated with cells followed by viral infection measured after 7 days by radioactive inc, EC50=0.0046μM 27405794
HepG2.2.15 Antiviral assay 3 days Antiviral activity against HBV infected in human HepG2.2.15 cells assessed as inhibition of viral DNA in cell supernatant incubated for 3 days in presence of 10% FBS followed by compound treatment in absence of 10% FBS for 3 days by qRT-PCR method, EC50=0.34μM 27405794
HepG2.2.15 Cytotoxicity assay 6 days Cytotoxicity against human HepG2.2.15 cells assessed as reduction in cell viability after 6 days by XTT assay, CC50=29.2μM 27405794
PBMC Antiviral assay 30 mins Antiviral activity against CXCR4-tropic HIV-1 NL4-3 infected in human PHA-stimulated PBMC assessed as inhibition of viral replication by measuring reduction in p24 antigen production preincubated with cells for 30 mins followed by viral infection measured, IC50=0.08μM 28682067
PBMC Antiviral assay 30 mins Antiviral activity against CCR5 tropic HIV1 BaL infected in human PHA-stimulated PBMC assessed as inhibition of viral replication by measuring reduction in p24 antigen production preincubated with cells for 30 mins followed by viral infection measured on , IC50=0.22μM 28682067
MT4 Antiviral assay 6 days Antiviral activity against CXCR4-tropic HIV-1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 6 days by XTT dye based assay, EC50=4.89μM 28682067
MT4 Antiviral assay 6 days Antiviral activity against tenofovir-resistant CXCR4-tropic HIV-1 NL4-3 harboring reverse transcriptase K65R mutant infected in human MT4 cells assessed as inhibition of viral replication inhibition of virus-induced cytopathic effect after 6 days by XTT d, EC50=11.3μM 28682067
HepG2.2.15 Antiviral assay Antiviral activity against HBV infected in human HepG2.2.15 cells assessed as reduction in cytoplasmic DNA synthesis by reed and munch method, IC50=0.85μM 31223460
HepG2.2.15 Cytotoxicity assay Cytotoxicity against human HepG2.2.15 cells infected with HBV, CC50=20.71μM 31223460
Click to View More Cell Line Experimental Data

Biological Activity

Description Tenofovir Disoproxil Fumarate 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.
Targets
HIV reverse transcriptase [1]
(Cell-free assay)
In vitro
In vitro

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. [1] 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. [2] 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. [3] 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. [4]
Cell Research Cell lines VK2 cells
Concentrations 450 μM or 1,350 μM
Incubation Time 15 min to 12 h
Method

VK2 cells were exposed to TDF (90 μM or 450 μM) and TFV (450 μM or 1,350 μM) in serum-free RPMI 1640 at 37°C for 15 min to 12 h. At different times postexposure, cells were washed with ice-cold PBS and metabolites were extracted overnight in 70% (vol/vol) methanol, followed by centrifugation at 18,000 × g for 10 min at 4°C. 
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05874440 Recruiting Chronic Hepatitis b Patients Sohag University April 15 2023 --
NCT03576066 Completed Chronic Hepatitis B Assembly Biosciences June 11 2018 Phase 2
NCT03361956 Completed Hepatitis B Janssen Sciences Ireland UC February 13 2018 Phase 2
NCT02985996 Completed HIV Infections Emory University|Centers for Disease Control and Prevention February 6 2017 Phase 1

Chemical lnformation & Solubility

Molecular Weight 635.51 Formula

C19H30N5O10P.C4H4O4
CAS No. 202138-50-9 SDF Download Tenofovir Disoproxil Fumarate SDF
Smiles CC(C)OC(=O)OCOP(=O)(COC(C)CN1C=NC2=C(N=CN=C21)N)OCOC(=O)OC(C)C.C(=CC(=O)O)C(=O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (157.35 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


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