Art. -Nr.: HY-13782A

Tenofovir Disoproxil

(Synonyms: Bis(POC)-PMPA; GS 4331)

12 Cited Publications

Kundenbewertung

Based on 12 publication(s) in Google Scholar

Tenofovir Disoproxil (Bis(POC)-PMPA) is a nucleotide reverse transcriptase inhibitor to treat HIV and chronic Hepatitis B.

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Reinheit: 99.52%
CAS. Nr.: 201341-05-1
Formel: C₁₉H₃₀N₅O₁₀P
Molecular Weight:519.44

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Tenofovir Disoproxil Chemical Structure

CAS. Nr.: 201341-05-1

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (12)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Tenofovir Disoproxil (Bis(POC)-PMPA) is a nucleotide reverse transcriptase inhibitor to treat HIV and chronic Hepatitis B.

IC₅₀ & Target

HIV-1

Alle HIV Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
CCRF-CEM	CC₅₀	>25 μM Compound: 12, Bis-POC-PMPA	Cytotoxicity against mock-infected human CEM cells assessed as growth inhibition Cytotoxicity against mock-infected human CEM cells assessed as growth inhibition	[PMID: 23603046]
CCRF-CEM	EC₅₀	0.013 μM Compound: 12, Bis-POC-PMPA	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	[PMID: 23603046]
CCRF-CEM	EC₅₀	0.016 μM Compound: 12, Bis-POC-PMPA	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	[PMID: 23603046]
HEL	EC₅₀	>50 μM Compound: 12, Bis-POC-PMPA	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	[PMID: 23603046]
HEL	EC₅₀	5.8 μM Compound: 12, Bis-POC-PMPA	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	[PMID: 23603046]
HEL	EC₅₀	5.8 μM Compound: 12, Bis-POC-PMPA	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	[PMID: 23603046]
HEL	EC₅₀	9.6 μM Compound: 12, Bis-POC-PMPA	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	[PMID: 23603046]
Huh-7	CC₅₀	>25 μM Compound: 12, Bis-POC-PMPA	Cytotoxicity against human HuH7 cells assessed as reduction of cell density Cytotoxicity against human HuH7 cells assessed as reduction of cell density	[PMID: 23603046]
Huh-7	EC₅₀	0.88 μM Compound: 12, Bis-POC-PMPA	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	[PMID: 23603046]
WI-38	CC₅₀	>50 μM Compound: Tenofovir disoproxil	Cytotoxicity against human WI38 cells by neutral red assay Cytotoxicity against human WI38 cells by neutral red assay	[PMID: 18285481]
WI-38	EC₅₀	>50 μM Compound: Tenofovir disoproxil	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	[PMID: 18285481]

In Vitro

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-1_BaL and X4-tropic HIV-1_IIIb 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-1_BaL, and is not toxic to PBMCs^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Tenofovir Disoproxil Fumarate (20, 50, 140, or 300 mg/kg) administered to BLT mice, shows dose dependent activity during vaginal HIV challenge in BLT humanized mice. Tenofovir Disoproxil Fumarate (50, 140, 300 mg/kg) significantly reduces HIV transmission in BLT mice^[3]. Tenofovir Disoproxil Fumarate (0.5, 1.5, or 5.0 mg/kg/day, p.o.) induces a dose-dependent decline in serum viremia in woodchucks chronically infected with WHV. Tenofovir Disoproxil Fumarate administration is safe and effective in the woodchuck model of chronic HBV infection^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 201341-05-1
Appearance Solid
Molecular Weight 519.44
Formel C₁₉H₃₀N₅O₁₀P
Color White to off-white
SMILES

O=C(OC(C)C)OCOP(OCOC(OC(C)C)=O)(CO[C@H](C)CN1C=NC2=C(N)N=CN=C12)=O
Synonyms

Bis(POC)-PMPA; GS 4331
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (12)

All WBIn Vivo Efficacy StudyRT-PCR

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Journal Impact Factor

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.
J Neuroimmune Pharmacol

Antiretroviral Drugs Promote Amyloidogenesis by De-Acidifying Endolysosomes. [Abstract]

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.
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

Efficacy of antiretroviral compounds against Toxoplasma gondii in vitro. [Abstract]

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 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.
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
SSRN

2026 Jun 23.
Res Sq

2026 Apr 3.
Charles University

2019 Jun.

Lösungsmittel & Löslichkeit

In Vitro:

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9252 mL

9.6258 mL

19.2515 mL

5 mM

0.3850 mL

1.9252 mL

3.8503 mL

10 mM

0.1925 mL

0.9626 mL

1.9252 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (4.00 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Protokoll

Cell Assay^[1]

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.

Animal Administration^[4]

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.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
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)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Tenofovir Disoproxil

12 Cited Publications

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Tenofovir Disoproxil

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Publications Citing Use of MedChemExpress (MCE) Tenofovir Disoproxil

Alle HIV Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (12)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Tenofovir Disoproxil

Anti-Infection Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

Antiviral Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Covalent Screening Library

Oxygen Sensing Compound Library

NMPA-Approved Drug Library

FDA Approved & Pharmacopeial Drug Library

Rare Diseases Drug Library

EMA-Approved Drug Library

FDA-Approved Anticancer Drug Library

Human Metabolite Library

Heterocyclic Compound Library

Off-patent Drug Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Nephrotoxicity Compound Library

Classic FDA-Approved Drug Library

Publications Citing Use of MedChemExpress (MCE) Tenofovir Disoproxil

Alle HIV Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (12)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Tenofovir Disoproxil Related Classifications

HY-13782A Related Classifications