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

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

Cat. No.: HY-13782A Purity: 99.84%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

Tenofovir Disoproxil Chemical Structure

CAS No. : 201341-05-1

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 55	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 55	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 32	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 100	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 140	In-stock	Estimated Time of Arrival: December 31
200 mg	USD 190	In-stock	Estimated Time of Arrival: December 31
500 mg	USD 280	In-stock	Estimated Time of Arrival: December 31
1 g		Get quote
5 g		Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 8 publication(s) in Google Scholar

Other Forms of Tenofovir Disoproxil:

Tenofovir Disoproxil fumarate In-stock
Tenofovir disoproxil aspartate Get quote

7 Publications Citing Use of MCE Tenofovir Disoproxil

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

: 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.

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All HIV Isoform Specific Products:

View All Isoforms

HIV HIV-1 HIV-2

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

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

IC₅₀ & Target

HIV-1

Cellular Effect

Cell Line	Type	Value	Description	References
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 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	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	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	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.

Clinical Trial

Molecular Weight

519.44

Formula

C₁₉H₃₀N₅O₁₀P

CAS No.

201341-05-1

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

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, 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.

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 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.
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.
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 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

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).

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: 99.84%

Select Batch:

Data Sheet (280 KB) SDS (392 KB)

COA (251 KB) LCMS (269 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]. 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]

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]. 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

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

Tenofovir Disoproxil Related Classifications

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 Disoproxil201341-05-1Bis(POC)-PMPA GS 4331GS4331GS 4331GS-4331HIVReverse TranscriptaseHBVHuman immunodeficiency virusHepatitis B virusInhibitorinhibitorinhibit

Please select a local distributor ナミキ商事株式会社コスモ・バイオ株式会社
Product Name			Salutation
Applicant Name *			Email Address *
Phone Number *			Organization Name *
Department *			Requested quantity *
Country or Region *
Remarks

Product Name			Lot #
Applicant Name *			Email Address *
Phone Number			Department *
Organization Name *			Country or Region *
Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

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

Customer Review

Other Forms of Tenofovir Disoproxil:

Tenofovir Disoproxil Related Antibodies

7 Publications Citing Use of MCE Tenofovir Disoproxil

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All HIV Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Tenofovir Disoproxil Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Tenofovir Disoproxil Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report