Art. -Nr.: HY-15232B

Tenofovir alafenamide hemifumarate

(Synonyms: GS-7340 hemifumarate)

11 Cited Publications

Kundenbewertung

Based on 11 publication(s) in Google Scholar

Tenofovir alafenamide hemifumarate (GS-7340 hemifumarate) is an investigational oral proagent of Tenofovir. Tenofovir is a HIV-1 nucleotide reverse transcriptase inhibitor.

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Reinheit: 99.92%
CAS. Nr.: 1392275-56-7
Formel: C₂₁H₂₉N₆O₅P.1/2 C₄H₄O₄
Molecular Weight:534.50

Speicherung:

4°C, sealed storage, away from moisture

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

Tenofovir alafenamide hemifumarate Chemical Structure

CAS. Nr.: 1392275-56-7

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (11)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Tenofovir alafenamide hemifumarate (GS-7340 hemifumarate) is an investigational oral proagent of Tenofovir. Tenofovir is a HIV-1 nucleotide reverse transcriptase inhibitor.

IC₅₀ & Target

HIV-1

HIV-2

Alle HIV Isoform-spezifische Produkte anzeigen :

In Vitro

Tenofovir alafenamide hemifumarate (GS-7340 hemifumarate) antiviral activities are similar across all cell types, ranging from 5 to 7 nM, while the CC₅₀ varies from 4.7 to 42 μM for MT-4 and MT-2 cells, respectively. The antiviral activity of TAF is evaluated against a panel of HIV-1 and HIV-2 isolates, including HIV-1 group M subtypes A to G, as well as group N and O isolates. Overall, for the 29 primary HIV-1 isolates tested in PBMCs, TAF EC₅₀s range from 0.1 to 12 nM, with a mean EC₅₀ of 3.5 nM compared to a mean EC₅₀ of 11.8 nM for AZT, which is used as an internal control. For the HIV-2 isolates, the mean EC₅₀s are 1.8 nM for TAF and 6.4 nM for AZT^[2].

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

In Vivo

Tenofovir alafenamide hemifumarate (GS-7340 hemifumarate) is an amidate prodrug of Tenofovir with good oral bioavailability and increases plasma stability compared to Tenofovir disoproxil fumarate (TDF) ^[1].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1392275-56-7
Appearance Solid
Molecular Weight 534.50
Formel C₂₁H₂₉N₆O₅P.1/2 C₄H₄O₄
Color White to off-white
SMILES

O=C(O)/C=C/C(O)=O.NC1=NC=NC2=C1N=CN2C[C@@H](C)OC[P@](OC3=CC=CC=C3)(N[C@@H](C)C(OC(C)C)=O)=O.[0.5]
Synonyms

GS-7340 hemifumarate
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

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

Publications (11)

All OthersCell Proliferation/Viability Assay

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Journal Impact Factor

J Med Chem

Differential Bioactivation Profiles of Different GS-441524 Prodrugs in Cell and Mouse Models: ProTide Prodrugs with High Cell Permeability and Susceptibility to Cathepsin A Are More Efficient in Delivering Antiviral Active Metabolites to the Lung. [Abstract]

2024 May 9;67(9):7470-7486. PMID: 38690769
Pharmaceutics

Activation of Tenofovir Alafenamide and Sofosbuvir in the Human Lung and Its Implications in the Development of Nucleoside/Nucleotide Prodrugs for Treating SARS-CoV-2 Pulmonary Infection. [Abstract]

2021 Oct 11;13(10):1656. PMID: 34683949

Tenofovir alafenamide hemifumarate purchased from MedChemExpress. Usage Cited in: Pharmaceutics. 2021 Oct 11;13(10):1656. [Abstract]

The activity of rhCES1 against TAF and SBV hydrolysis was assessed. 40 ng/µL rhCES1 was incubated with 20 µM TAF or SBV at 37 °C for 5 min and 20 min, respectively.
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

Non-nucleoside hepatitis B virus polymerase inhibitors identified by an in vitro polymerase elongation assay. [Abstract]

2020 Apr;55(4):441-452 PMID: 31768802

Tenofovir alafenamide hemifumarate purchased from MedChemExpress. Usage Cited in: J Gastroenterol. 2020 Apr;55(4):441-452 [Abstract]

HepG2.2.15.7 cells were cultured for 6 days with or without a specified concentration of PDM2, and treated with or without Tenofovir alafenamide (TAF). Cell viability was determined using the MTT assay.
ACS Infect Dis

Targeting the Rift Valley Fever Virus Polymerase: Resistance Mechanisms and Structural Insights. [Abstract]

2025 Oct 30. PMID: 41166549
Antimicrob Agents Chemother

CMCdG, a Novel Nucleoside Analog with Favorable Safety Features, Exerts Potent Activity against Wild-Type and Entecavir-Resistant Hepatitis B Virus. [Abstract]

2019 Mar 27;63(4):e02143-18. PMID: 30670420
J Antimicrob Chemother

Single-dose pharmacokinetics of tenofovir alafenamide and its active metabolite in the mucosal tissues. [Abstract]

2017 Jun 1;72(6):1731-1740. PMID: 28369415
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
J Chromatogr B Analyt Technol Biomed Life Sci

Development, validation and clinical implementation of a HPLC-MS/MS method for the simultaneous quantification of bictegravir, emtricitabine, doravirine, cabotegravir, lenacapavir, fostemsavir, tenofovir alafenamide and the corresponding metabolites temsavir and tenofovir, in human plasma. [Abstract]

2025 Dec 15:1267:124803. PMID: 41072339
Preprints

2024 Apr 19.
Research Square Print

2023 Mar 20.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (93.55 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 20 mg/mL (37.42 mM; ultrasonic and warming and heat to 60°C)

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

1.8709 mL

9.3545 mL

18.7091 mL

5 mM

0.3742 mL

1.8709 mL

3.7418 mL

10 mM

0.1871 mL

0.9355 mL

1.8709 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* 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.

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: ≥ 2.5 mg/mL (4.68 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (4.68 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 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: 2.5 mg/mL (4.68 mM); Clear solution; Need warming

This protocol yields a clear solution of 2.5 mg/mL. 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.

Working 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.

Protocol 1

Add each solvent one by one: PBS

Solubility: 4.55 mg/mL (8.51 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

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.

Working solution concentration: 0.22 mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

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) .

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 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]. Birkus G, et al. Intracellular Activation of Tenofovir Alafenamide and the Effect of Viral and Host Protease Inhibitors. Antimicrob Agents Chemother. 2015 Oct 26;60(1):316-22. [Content Brief]

[2]. Callebaut C, et al. In Vitro Virology Profile of Tenofovir Alafenamide, a Novel Oral Prodrug of Tenofovir with Improved Antiviral Activity Compared to That of Tenofovir Disoproxil Fumarate. Antimicrob Agents Chemother. 2015 Oct;59(10):5909-16. [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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
H₂O / DMSO	1 mM	1.8709 mL	9.3545 mL	18.7091 mL	46.7727 mL
	5 mM	0.3742 mL	1.8709 mL	3.7418 mL	9.3545 mL
	10 mM	0.1871 mL	0.9355 mL	1.8709 mL	4.6773 mL
	15 mM	0.1247 mL	0.6236 mL	1.2473 mL	3.1182 mL
	20 mM	0.0935 mL	0.4677 mL	0.9355 mL	2.3386 mL
	25 mM	0.0748 mL	0.3742 mL	0.7484 mL	1.8709 mL
	30 mM	0.0624 mL	0.3118 mL	0.6236 mL	1.5591 mL
DMSO	40 mM	0.0468 mL	0.2339 mL	0.4677 mL	1.1693 mL
	50 mM	0.0374 mL	0.1871 mL	0.3742 mL	0.9355 mL
	60 mM	0.0312 mL	0.1559 mL	0.3118 mL	0.7795 mL
	80 mM	0.0234 mL	0.1169 mL	0.2339 mL	0.5847 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.

Keywords

Tenofovir alafenamide hemifumarate

11 Cited Publications

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Tenofovir alafenamide hemifumarate

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Publications Citing Use of MedChemExpress (MCE) Tenofovir alafenamide hemifumarate

Alle HIV Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (11)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Tenofovir alafenamide hemifumarate

Anti-Infection Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

Antiviral Compound Library

Drug Repurposing Compound Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Rare Diseases Drug Library

EMA-Approved Drug Library

FDA-Approved Anticancer Drug Library

Non-steroidal Anti-Inflammatory Compound Library

Off-patent Drug Library

Multi-Target Compound Library

Bioactive Compound Library Max

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Tenofovir alafenamide hemifumarate

Alle HIV Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (11)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Tenofovir alafenamide hemifumarate Related Classifications

HY-15232B Related Classifications