Tenofovir Disoproxil
Based on 11 publication(s) in Google Scholar
Tenofovir Disoproxil (Bis(POC)-PMPA) is a nucleotide reverse transcriptase inhibitor to treat HIV and chronic Hepatitis B.
For research use only. We do not sell to patients.
- Purity: 99.52%
- CAS No.: 201341-05-1
- Formula: C19H30N5O10P
- Molecular Weight:519.44
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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
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Publications Citing Use of MedChemExpress (MCE) Tenofovir Disoproxil
More- Cell. 2025 Sep 4;188(18):4896-4912.e19. [Abstract]
- Adv Sci (Weinh). 2024 Aug 19:e2403058. [Abstract]
- J Gastroenterol. 2021 Feb;56(2):168-180. [Abstract]
- Pharmaceuticals (Basel). 2025 Oct 16;18(10):1560. [Abstract]
- Int J Antimicrob Agents. 2019 Dec;54(6):814-819. [Abstract]
- Drug Metab Dispos. 2026 Mar 2;54(5):100263. [Abstract]
- Sci Rep. 2019 Nov 20;9(1):17158. [Abstract]
- J Neuroimmune Pharmacol. 2021 Mar;16(1):159-168. [Abstract]
- J Neuroimmune Pharmacol. 2017 Dec;12(4):682-692. [Abstract]
- SSRN. 2026 Jun 23.
- Charles University. 2019 Jun.
Customer Validation & Images
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RT-PCR
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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 |
|---|---|---|---|---|
| CCRF-CEM | CC50 |
>25 μM
Compound: 12, Bis-POC-PMPA
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Cytotoxicity against mock-infected human CEM cells assessed as growth inhibition
Cytotoxicity against mock-infected human CEM cells assessed as growth inhibition
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[PMID: 23603046] |
| CCRF-CEM | EC50 |
0.013 μM
Compound: 12, Bis-POC-PMPA
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Antiviral activity against wild type HIV-2 ROD infected in human CEM cells assessed as inhibition of syncytia formation after 4 days by microscopic analysis
Antiviral activity against wild type HIV-2 ROD infected in human CEM cells assessed as inhibition of syncytia formation after 4 days by microscopic analysis
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[PMID: 23603046] |
| CCRF-CEM | EC50 |
0.016 μM
Compound: 12, Bis-POC-PMPA
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Antiviral activity against wild type HIV-1 3B infected in human CEM cells assessed as inhibition of syncytia formation after 4 days by microscopic analysis
Antiviral activity against wild type HIV-1 3B infected in human CEM cells assessed as inhibition of syncytia formation after 4 days by microscopic analysis
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[PMID: 23603046] |
| HEL | EC50 |
>50 μM
Compound: 12, Bis-POC-PMPA
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Antiviral activity against Vaccinia virus infected in human HEL cells assessed as reduction of virus-induced cytopathicity measured at day 3 by microscopic analysis
Antiviral activity against Vaccinia virus infected in human HEL cells assessed as reduction of virus-induced cytopathicity measured at day 3 by microscopic analysis
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[PMID: 23603046] |
| HEL | EC50 |
5.8 μM
Compound: 12, Bis-POC-PMPA
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Antiviral activity against Human simplex virus 1 KOS infected in human HEL cells assessed as reduction of virus-induced cytopathicity measured at day 3 by microscopic analysis
Antiviral activity against Human simplex virus 1 KOS infected in human HEL cells assessed as reduction of virus-induced cytopathicity measured at day 3 by microscopic analysis
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[PMID: 23603046] |
| HEL | EC50 |
5.8 μM
Compound: 12, Bis-POC-PMPA
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Antiviral activity against Human simplex virus 2 G infected in human HEL cells assessed as reduction of virus-induced cytopathicity measured at day 3 by microscopic analysis
Antiviral activity against Human simplex virus 2 G infected in human HEL cells assessed as reduction of virus-induced cytopathicity measured at day 3 by microscopic analysis
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[PMID: 23603046] |
| HEL | EC50 |
9.6 μM
Compound: 12, Bis-POC-PMPA
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Antiviral activity against thymidine kinase-deficient Human simplex virus 1 KOS infected in human HEL cells assessed as reduction of virus-induced cytopathicity measured at day 3 by microscopic analysis
Antiviral activity against thymidine kinase-deficient Human simplex virus 1 KOS infected in human HEL cells assessed as reduction of virus-induced cytopathicity measured at day 3 by microscopic analysis
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[PMID: 23603046] |
| Huh-7 | CC50 |
>25 μM
Compound: 12, Bis-POC-PMPA
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Cytotoxicity against human HuH7 cells assessed as reduction of cell density
Cytotoxicity against human HuH7 cells assessed as reduction of cell density
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[PMID: 23603046] |
| Huh-7 | EC50 |
0.88 μM
Compound: 12, Bis-POC-PMPA
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Antiviral activity against wild type HBV transfected in human HuH7 cells assessed as reduction of viral DNA level after 7 days by qPCR analysis
Antiviral activity against wild type HBV transfected in human HuH7 cells assessed as reduction of viral DNA level after 7 days by qPCR analysis
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[PMID: 23603046] |
| WI-38 | CC50 |
>50 μM
Compound: Tenofovir disoproxil
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Cytotoxicity against human WI38 cells by neutral red assay
Cytotoxicity against human WI38 cells by neutral red assay
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[PMID: 18285481] |
| WI-38 | EC50 |
>50 μM
Compound: Tenofovir disoproxil
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Antimicrobial activity against BK polyomavirus ATCC VR837 infected in human WI38 cells assessed as reduction in viral titer after 7 days by PCR analysis
Antimicrobial activity against BK polyomavirus ATCC VR837 infected in human WI38 cells assessed as reduction in viral titer after 7 days by PCR analysis
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[PMID: 18285481] |
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.
Chemical Information
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CAS No. 201341-05-1
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Appearance Solid
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Molecular Weight 519.44
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Formula C19H30N5O10P
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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
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Synonyms
Bis(POC)-PMPA; GS 4331
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (11)
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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 Aug 19:e2403058. PMID: 39159293
Tenofovir Disoproxil purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Aug 19: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 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Aug 19: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 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Aug 19: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 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 -
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 -
Int J Antimicrob Agents
2019 Dec;54(6):814-819. PMID: 31479744 -
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 -
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 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 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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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 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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Solvent & Solubility
DMSO : ≥ 38 mg/mL (73.16 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.00 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.00 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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.
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 (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 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]. 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]
[3]. 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]
[4]. 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9252 mL | 9.6258 mL | 19.2515 mL | 48.1288 mL |
| 5 mM | 0.3850 mL | 1.9252 mL | 3.8503 mL | 9.6258 mL | |
| 10 mM | 0.1925 mL | 0.9626 mL | 1.9252 mL | 4.8129 mL | |
| 15 mM | 0.1283 mL | 0.6417 mL | 1.2834 mL | 3.2086 mL | |
| 20 mM | 0.0963 mL | 0.4813 mL | 0.9626 mL | 2.4064 mL | |
| 25 mM | 0.0770 mL | 0.3850 mL | 0.7701 mL | 1.9252 mL | |
| 30 mM | 0.0642 mL | 0.3209 mL | 0.6417 mL | 1.6043 mL | |
| 40 mM | 0.0481 mL | 0.2406 mL | 0.4813 mL | 1.2032 mL | |
| 50 mM | 0.0385 mL | 0.1925 mL | 0.3850 mL | 0.9626 mL | |
| 60 mM | 0.0321 mL | 0.1604 mL | 0.3209 mL | 0.8021 mL |
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