Tenofovir Disoproxil fumarate (Synonyms: Tenofovir DF; Bis(POC)-PMPA fumarate; GS 4331 fumarate)

Name: Tenofovir Disoproxil fumarate
Brand: MedChemExpress
SKU: HY-13782
Rating: 5.0 (8 reviews)

Cat. No.: HY-13782 Purity: 99.67%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

Tenofovir Disoproxil fumarate Chemical Structure

CAS No. : 202138-50-9

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Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 61	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 61	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 35	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 55	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 110	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 154	In-stock	Estimated Time of Arrival: December 31
200 mg	USD 209	In-stock	Estimated Time of Arrival: December 31
500 mg	USD 308	In-stock	Estimated Time of Arrival: December 31
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Based on 8 publication(s) in Google Scholar

Other Forms of Tenofovir Disoproxil fumarate:

Tenofovir In-stock
Tenofovir Disoproxil In-stock
Tenofovir maleate Get quote
Tenofovir disoproxil aspartate Get quote
Tenofovir Disoproxil fumarate (Standard) Get quote

7 Publications Citing Use of MCE Tenofovir Disoproxil fumarate

•Department od Analytical Chemistry, Charles University. 2019 Jun.

: 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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HIV HIV-1 HIV-2

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

Tenofovir Disoproxil fumarate is a nucleotide reverse transcriptase inhibitor used to treat HIV and chronic Hepatitis B.

IC₅₀ & Target

HIV-1

Cellular Effect

Cell Line	Type	Value	Description	References
Bone marrow cell	CC₅₀	0.9 μM Compound: TDF	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	[PMID: 20439609]
Bone marrow cell	CC₅₀	1.9 μM Compound: TDF	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	[PMID: 20439609]
HepG2	IC₅₀	2.31 μM Compound: Tenofovir DF	Cytotoxicity against human HepG2 cells after 9 days by MTT assay Cytotoxicity against human HepG2 cells after 9 days by MTT assay	[PMID: 17888662]
HepG2	IC₅₀	5.1 μM Compound: Tenofovir DF	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	[PMID: 17888662]
HepG2	CC₅₀	64.5 μM Compound: TDF	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	[PMID: 27933889]
HepG2 2.2.15	CC₅₀	29.2 μM Compound: TDF	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	[PMID: 27405794]
MT2	EC₅₀	0.015 μM Compound: 1, Tenofovir DF	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	[PMID: 17562366]
MT2	EC₅₀	6.8 nM Compound: TDF	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	[PMID: 19104010]
MT4	CC₅₀	> 20 μM Compound: TDF	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	[PMID: 28682067]
PBMC	CC₅₀	14.56 μM Compound: TDF	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	[PMID: 28682067]
PBMC	CC₅₀	43.7 μM Compound: TDF	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	[PMID: 27405794]
PBMC	CC₅₀	44 μM Compound: TDF	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	[PMID: 27933889]

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.

Clinical Trial

Molecular Weight

635.51

Formula

C₂₃H₃₄N₅O₁₄P

CAS No.

202138-50-9

Appearance

Solid

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.O=C(O)/C=C/C(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

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.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.5735 mL	7.8677 mL	15.7354 mL
5 mM	0.3147 mL	1.5735 mL	3.1471 mL
10 mM	0.1574 mL	0.7868 mL	1.5735 mL

View the 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.

* 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Protocol 1

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.
Protocol 2

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (3.93 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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.

Protocol 1

Add each solvent one by one: PBS
Solubility: 20 mg/mL (31.47 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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

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).

Calculation results:

Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.67%

Select Batch:

Data Sheet (279 KB) SDS (393 KB)

COA (248 KB) LCMS (268 KB)

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]

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

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

Infection

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Tenofovir Disoproxil202138-50-9Tenofovir DFBis(POC)-PMPAGS 4331GS4331GS-4331HIVReverse TranscriptaseHBVHuman immunodeficiency virusHepatitis B virusInhibitorinhibitorinhibit

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Tenofovir Disoproxil fumarate (Synonyms: Tenofovir DF; Bis(POC)-PMPA fumarate; GS 4331 fumarate)

Customer Review

Other Forms of Tenofovir Disoproxil fumarate:

Tenofovir Disoproxil fumarate Related Antibodies

7 Publications Citing Use of MCE Tenofovir Disoproxil fumarate

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•Related Screening Libraries:

•Related Small Molecules:

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View All HIV Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Tenofovir Disoproxil fumarate Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Tenofovir Disoproxil fumarate Related Classifications

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