Tenofovir alafenamide hemifumarate
Based on 12 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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- Pureté: 99.92%
- CAS No.: 1392275-56-7
- Formule: C21H29N6O5P.1/2 C4H4O4
- Masse moléculaire:534.50
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Tenofovir alafenamide hemifumarate
More- J Med Chem. 2024 May 9;67(9):7470-7486. [Abstract]
- Pharmaceutics. 2021 Oct 11;13(10):1656. [Abstract]
- Pharmaceuticals (Basel). 2025 Oct 16;18(10):1560. [Abstract]
- J Gastroenterol. 2020 Apr;55(4):441-452. [Abstract]
- ACS Infect Dis. 2025 Oct 30. [Abstract]
- Antimicrob Agents Chemother. 2019 Mar 27;63(4):e02143-18. [Abstract]
- J Antimicrob Chemother. 2017 Jun 1;72(6):1731-1740. [Abstract]
- Drug Metab Dispos. 2026 Mar 2;54(5):100263. [Abstract]
- J Chromatogr B Analyt Technol Biomed Life Sci. 2025 Dec 15:1267:124803. [Abstract]
- SSRN. 2026 Jun 24.
- Preprints. 2024 Apr 19.
- Research Square Print. 2023 Mar 20.
Customer Validation & Images
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Others
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Cell Proliferation/Viability Assay
Activité biologique
Description
IC50 & Target
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HIV-1 |
HIV-2 |
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
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1392275-56-7
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Appearance Solid
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Masse moléculaire 534.50
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Formule C21H29N6O5P.1/2 C4H4O4
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Color White to off-white
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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]
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Synonyms
GS-7340 hemifumarate
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (12)
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Journal Impact Factor
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Most Recent
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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.
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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.
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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 -
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Solvant et solubilité
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)
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.
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.
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.
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.
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: ≥ 2.5 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.
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.
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.
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:
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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.
Pureté et documentation
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Fiche technique (281 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)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[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]
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, 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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| 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.
Tenofovir alafenamide hemifumarate Related Classifications
HY-15232B Related Classifications
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