Tenofovir Disoproxil fumarate
Based on 12 publication(s) in Google Scholar
Tenofovir Disoproxil fumarate is a nucleotide reverse transcriptase inhibitor used to treat HIV and chronic Hepatitis B.
For research use only. We do not sell to patients.
- Purity: 99.62%
- CAS No.: 202138-50-9
- Formula: C23H34N5O14P
- Molecular Weight:635.51
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Tenofovir Disoproxil fumarate
More- Cell. 2025 Sep 4;188(18):4896-4912.e19. [Abstract]
- Adv Sci (Weinh). 2024 Oct;11(39):e2403058. [Abstract]
- J Neuroimmune Pharmacol. 2021 Mar;16(1):159-168. [Abstract]
- J Neuroimmune Pharmacol. 2017 Dec;12(4):682-692. [Abstract]
- Pharmaceuticals (Basel). 2025 Oct 16;18(10):1560. [Abstract]
- J Gastroenterol. 2021 Feb;56(2):168-180. [Abstract]
- Int J Antimicrob Agents. 2019 Dec;54(6):814-819. [Abstract]
- Sci Rep. 2019 Nov 20;9(1):17158. [Abstract]
- Drug Metab Dispos. 2026 Mar 2;54(5):100263. [Abstract]
- SSRN. 2026 Jun 23.
- Res Sq. 2026 Apr 3.
- Charles University. 2019 Jun.
Customer Validation & Images
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WB
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RT-PCR
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WB
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In Vivo Efficacy Study
Biological Activity
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HIV-1 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Bone marrow cell | CC50 |
0.9 μM
Compound: TDF
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Cytotoxicity against human bone marrow cells after 24 hrs by BFU-E assay
Cytotoxicity against human bone marrow cells after 24 hrs by BFU-E assay
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[PMID: 20439609] |
| Bone marrow cell | CC50 |
1.9 μM
Compound: TDF
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Cytotoxicity against human bone marrow cells after 24 hrs by GM-CFU assay
Cytotoxicity against human bone marrow cells after 24 hrs by GM-CFU assay
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[PMID: 20439609] |
| CCRF-CEM | CC50 |
>5 μM
Compound: TDF
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Cytotoxicity against human CEM cells assessed as inhibition of cell proliferation
Cytotoxicity against human CEM cells assessed as inhibition of cell proliferation
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[PMID: 38086193] |
| HeLa | IC50 |
11.4 μM
Compound: TDF
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Antiviral activity against HIV1 harboring reverse transcriptase K65R mutant infected in human HeLa P4/R5 cells assessed as inhibition of viral replication
Antiviral activity against HIV1 harboring reverse transcriptase K65R mutant infected in human HeLa P4/R5 cells assessed as inhibition of viral replication
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[PMID: 19596885] |
| HeLa | IC50 |
4.7 μM
Compound: TDF
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Antiviral activity against HIV1 infected in human HeLa P4/R5 cells assessed as inhibition of viral replication
Antiviral activity against HIV1 infected in human HeLa P4/R5 cells assessed as inhibition of viral replication
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[PMID: 19596885] |
| HepG2 | CC50 |
64.5 μM
Compound: TDF
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Cytotoxicity in uninfected human hepG2 assessed as reduction in cell viability by XTT assay
Cytotoxicity in uninfected human hepG2 assessed as reduction in cell viability by XTT assay
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[PMID: 27933889] |
| HepG2 | IC50 |
2.31 μM
Compound: Tenofovir DF
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Cytotoxicity against human HepG2 cells after 9 days by MTT assay
Cytotoxicity against human HepG2 cells after 9 days by MTT assay
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[PMID: 17888662] |
| HepG2 | IC50 |
5.1 μM
Compound: Tenofovir DF
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Antiviral activity against Hepatitis B virus infected human HepG2 cells after 9 days by MTT assay
Antiviral activity against Hepatitis B virus infected human HepG2 cells after 9 days by MTT assay
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[PMID: 17888662] |
| HepG2 2.2.15 | CC50 |
20.71 μM
Compound: TDF
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Cytotoxicity against human HepG2.2.15 cells infected with HBV
Cytotoxicity against human HepG2.2.15 cells infected with HBV
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[PMID: 31223460] |
| HepG2 2.2.15 | CC50 |
29.2 μM
Compound: TDF
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Cytotoxicity against human HepG2.2.15 cells assessed as reduction in cell viability after 6 days by XTT assay
Cytotoxicity against human HepG2.2.15 cells assessed as reduction in cell viability after 6 days by XTT assay
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[PMID: 27405794] |
| MT2 | CC50 |
>50 μM
Compound: 1, Tenofovir DF
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Cytotoxicity against MT2 cells
Cytotoxicity against MT2 cells
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[PMID: 17562366] |
| MT2 | EC50 |
0.015 μM
Compound: 1, Tenofovir DF
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Inhibition of virus-induced cytopathic effect in wild type HIV 3a infected MT2 cells after 5 days
Inhibition of virus-induced cytopathic effect in wild type HIV 3a infected MT2 cells after 5 days
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[PMID: 17562366] |
| MT2 | EC50 |
6.8 nM
Compound: TDF
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Antiviral activity against HIV1 3B infected in human MT-2 cells by two fold dilution method in presence of 10% FBS
Antiviral activity against HIV1 3B infected in human MT-2 cells by two fold dilution method in presence of 10% FBS
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[PMID: 19104010] |
| MT2 | IC50 |
0.54 μM
Compound: TDF
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Antiviral activity against HIV1 infected in human MT2 cells assessed as inhibition of viral replication
Antiviral activity against HIV1 infected in human MT2 cells assessed as inhibition of viral replication
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[PMID: 19596885] |
| MT4 | CC50 |
>20 μM
Compound: TDF
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Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 6 days by XTT tetrazolium dye-based assay
Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 6 days by XTT tetrazolium dye-based assay
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[PMID: 28682067] |
| PBMC | CC50 |
14.56 μM
Compound: TDF
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Cytotoxicity against human PHA-stimulated PBMC assessed as cell viability by tetrazolium dye assay
Cytotoxicity against human PHA-stimulated PBMC assessed as cell viability by tetrazolium dye assay
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[PMID: 28682067] |
| PBMC | CC50 |
43.7 μM
Compound: TDF
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Cytotoxicity against human PBMC assessed as reduction in cell viability by XTT assay
Cytotoxicity against human PBMC assessed as reduction in cell viability by XTT assay
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[PMID: 27405794] |
| PBMC | CC50 |
44 μM
Compound: TDF
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Cytotoxicity in uninfected human PBMC assessed as reduction in cell viability by XTT assay
Cytotoxicity in uninfected human PBMC assessed as reduction in cell viability by XTT assay
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[PMID: 27933889] |
Tenofovir shows cytotoxic effects on cell viability in HK-2 cells, with IC50 values of 9.21 and 2.77 μM at 48 and 72 h in MTT assay, respectively. Tenofovir diminishes ATP levels in HK-2 cells. Tenofovir (3.0 to 28.8 μM) increases oxidative stress and protein carbonylation in HK-2 cells. Furthermore, Tenofovir induces apoptosis in HK-2 cells, and that apoptosis is induced via mitochondrial damage[1]. Tenofovir and M48U1 formulated in 0.25% HEC each inhibits the replication of both R5-tropic HIV-1BaL and X4-tropic HIV-1IIIb in activated PBMCs, and inhibits several laboratory strains and patient-derived HIV-1 isolates. The combined formulation of M48U1 and tenofovir in 0.25% HEC exhibits synergistic antiretroviral activity against infection with R5-tropic HIV-1BaL, and is not toxic to PBMCs[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 202138-50-9
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Appearance Solid
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Molecular Weight 635.51
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Formula C23H34N5O14P
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Color White to off-white
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SMILES
O=C(OC(C)C)OCOP(OCOC(OC(C)C)=O)(CO[C@H](C)CN1C=NC2=C(N)N=CN=C12)=O.O=C(O)/C=C/C(O)=O
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Synonyms
Tenofovir DF; Bis(POC)-PMPA fumarate; GS 4331 fumarate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
Publications (12)
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Journal Impact Factor
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Most Recent
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Cell
Combination antiretroviral therapy and MCL-1 inhibition mitigate HTLV-1 infection in vivo. [Abstract]2025 Sep 4;188(18):4896-4912.e19. PMID: 40645177 -
Adv Sci (Weinh)
Ginsenoside Rg3 Restores Mitochondrial Cardiolipin Homeostasis via GRB2 to Prevent Parkinson's Disease. [Abstract]2024 Oct;11(39):e2403058. PMID: 39159293
Tenofovir Disoproxil fumarate purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Oct;11(39):e2403058. [Abstract]
SH-SY5Y cells were stimulated with Tenofovir Disoproxil fumarate (TDF, 10 µM) or DMSO (0.1%) for 24 h. Western blotting was performed to evaluate the expression of TRKA and EGFR in cell lysates immunoprecipitated with an anti-GRB2 antibody.
Tenofovir Disoproxil fumarate purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Oct;11(39):e2403058. [Abstract]
SH-SY5Y cells were stimulated with Tenofovir Disoproxil fumarate (TDF, 10 µM) or DMSO (0.1%) for 24 h. Quantification of TRKA levels.
Tenofovir Disoproxil fumarate purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Oct;11(39):e2403058. [Abstract]
SH-SY5Y cells were stimulated with TDF (10 µM) or DMSO (0.1%) for 24 h. Representative western blot images of CRLS1, GRB2, TRKA in SH-SY5Y cells treated with Tenofovir Disoproxil fumarate (TDF, 10 µM) or DMSO (0.1%) for 24 h after transfection with Scramble, GRB2 or TRKA siRNAs for 24 h.
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J Neuroimmune Pharmacol
2021 Mar;16(1):159-168. PMID: 31338753 -
J Neuroimmune Pharmacol
Combined Medication of Antiretroviral Drugs Tenofovir Disoproxil Fumarate, Emtricitabine, and Raltegravir Reduces Neural Progenitor Cell Proliferation In Vivo and In Vitro. [Abstract]2017 Dec;12(4):682-692. PMID: 28735382
Tenofovir Disoproxil fumarate purchased from MedChemExpress. Usage Cited in: J Neuroimmune Pharmacol. 2017 Dec;12(4):682-692. [Abstract]
TDF/FTC/RAL combined medication induces mouse NPC apoptosis in vitro. Mouse NPCs are treated with either DMSO or TDF/FTC/RAL for 8 h. Cleaved Caspase-3 levels are determined by Western blotting.
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Pharmaceuticals (Basel)
New Assay Systems to Characterize the Broad-Spectrum Antiherpesviral and Non-Herpesviral Activity of Cyclin-Dependent Kinase (CDK) 8 Inhibitors. [Abstract]2025 Oct 16;18(10):1560. PMID: 41155676 -
J Gastroenterol
Tenofovir-disoproxil-fumarate modulates lipid metabolism via hepatic CD36/PPAR-alpha activation in hepatitis B virus infection. [Abstract]2021 Feb;56(2):168-180. PMID: 33211179 -
Int J Antimicrob Agents
2019 Dec;54(6):814-819. PMID: 31479744 -
Sci Rep
Tenofovir disoproxil fumarate induces peripheral neuropathy and alters inflammation and mitochondrial biogenesis in the brains of mice. [Abstract]2019 Nov 20;9(1):17158. PMID: 31748578
Tenofovir Disoproxil fumarate purchased from MedChemExpress. Usage Cited in: Sci Rep. 2019 Nov 20;9(1):17158. [Abstract]
MAP2 signal was as expected in wt mice, being noted throughout neuronal soma and processes, but in vehicle-treated gp120-tg and gp120-tg mice treated with Tenofovir Disoproxil fumarate (TDF) the MAP2 signal was greatly diminished suggesting loss of neuronal integrity.
Tenofovir Disoproxil fumarate purchased from MedChemExpress. Usage Cited in: Sci Rep. 2019 Nov 20;9(1):17158. [Abstract]
In the wt group, treatment with Tenofovir Disoproxil fumarate (TDF) led to a significant increase in GFAP optical density compared to the vehicle treated group, but this TDF-mediated increase was not seen in the GP120-tg group.
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Drug Metab Dispos
A minimal physiologically based pharmacokinetic model for predicting the metabolism of tenofovir prodrugs in the liver of human with fibrosis. [Abstract]2026 Mar 2;54(5):100263. PMID: 42085925 -
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Solvent & Solubility
DMSO : ≥ 50 mg/mL (78.68 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 10 mg/mL (15.74 mM; ultrasonic and warming and heat to 60°C)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (7.87 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.93 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 20 mg/mL (31.47 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
Cells are plated into 48-well tissue culture plates (39,000 cells/mL) and allowed to grow for 48 h followed by treatment with vehicle or Tenofovir. Following the treatment period, cell viability is assessed using the MTT assay. The MTT assay relies on the conversion of tetrazolium dye 3-(4,5-dimethlthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) to formazan by NAD(P)H-dependent oxidoreductases.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Twenty adult chronic WHV carrier woodchucks are stratified equally by age, sex, body weight, and serum GGT activity into five treatment groups consisting of four animals each: (i) Tenofovir Disoproxil fumarate at 15.0 mg/kg once per day, (ii) Tenofovir Disoproxil fumarate at 5.0 mg/kg/day, (iii) Tenofovir Disoproxil fumarate at 1.5 mg/kg/day, (iv) Tenofovir Disoproxil fumarate at 0.5 mg/kg/day, and (v) a placebo control. The woodchucks are treated daily for 4 weeks and observed for an additional 12 weeks following cessation of drug treatment.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (279 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
[1]. Murphy RA, et al. Establishment of HK-2 Cells as a Relevant Model to Study Tenofovir-Induced Cytotoxicity. Int J Mol Sci. 2017 Mar 1;18(3) [Content Brief]
[2]. Xu P, et al. Combined Medication of Antiretroviral Drugs Tenofovir Disoproxil Fumarate, Emtricitabine, and Raltegravir Reduces Neural Progenitor Cell Proliferation In Vivo and In Vitro. J Neuroimmune Pharmacol. 2017 Dec;12(4):682-692. [Content Brief]
[3]. Musumeci G, et al. M48U1 and Tenofovir combination synergistically inhibits HIV infection in activated PBMCs and human cervicovaginal histocultures. Sci Rep. 2017 Feb 1;7:41018 [Content Brief]
[4]. Wahl A, et al. Predicting HIV Pre-exposure Prophylaxis Efficacy for Women using a Preclinical Pharmacokinetic-Pharmacodynamic In Vivo Model. Sci Rep. 2017 Feb 1;7:41098 [Content Brief]
[5]. Menne S, Cote PJ, Korba BE, Antiviral effect of oral administration of tenofovir disoproxil fumarate in woodchucks with chronic woodchuck hepatitis virus infection. Antimicrob Agents Chemother. 2005 Jul;49(7):2720-8. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 1.5735 mL | 7.8677 mL | 15.7354 mL | 39.3385 mL |
| 5 mM | 0.3147 mL | 1.5735 mL | 3.1471 mL | 7.8677 mL | |
| 10 mM | 0.1574 mL | 0.7868 mL | 1.5735 mL | 3.9338 mL | |
| 15 mM | 0.1049 mL | 0.5245 mL | 1.0490 mL | 2.6226 mL | |
| DMSO | 20 mM | 0.0787 mL | 0.3934 mL | 0.7868 mL | 1.9669 mL |
| 25 mM | 0.0629 mL | 0.3147 mL | 0.6294 mL | 1.5735 mL | |
| 30 mM | 0.0525 mL | 0.2623 mL | 0.5245 mL | 1.3113 mL | |
| 40 mM | 0.0393 mL | 0.1967 mL | 0.3934 mL | 0.9835 mL | |
| 50 mM | 0.0315 mL | 0.1574 mL | 0.3147 mL | 0.7868 mL | |
| 60 mM | 0.0262 mL | 0.1311 mL | 0.2623 mL | 0.6556 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Tenofovir Disoproxil fumarate Related Classifications
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