Tenofovir alafenamide
Based on 12 publication(s) in Google Scholar
Tenofovir alafenamide (GS-7340) is an investigational oral proagent of Tenofovir. Tenofovir is a HIV-1 nucleotide reverse transcriptase inhibitor.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.93%
- No. CAS: 379270-37-8
- Fòrmula: C21H29N6O5P
- Peso molecular:476.47
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) Tenofovir alafenamide
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]
- Preprints. 2024 Apr 19.
- Research Square Print. 2023 Mar 20.
- Univerzita Karlova v Praz. 2021 Jun.
Customer Validation & Images
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Others
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Cell Proliferation/Viability Assay
Actividad biológica
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HIV-1 |
HIV-2 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 2.2.15 | CC50 |
>100 μM
Compound: GS-7340
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Cytotoxicity against human HepG2.2.15 cells assessed as reduction in cell viability treated from day 2 to day 8 by CellTiter-Blue reagent based fluorescence analysis
Cytotoxicity against human HepG2.2.15 cells assessed as reduction in cell viability treated from day 2 to day 8 by CellTiter-Blue reagent based fluorescence analysis
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[PMID: 38246114] |
| MT2 | CC50 |
40 μM
Compound: GS 7340
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Cytotoxicity against human MT2 cells
Cytotoxicity against human MT2 cells
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[PMID: 24686012] |
| MT2 | EC50 |
0.005 μM
Compound: GS 7340
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Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT2 cells assessed as inhibition of virus-induced giant cell formation after 4 to 5 days by microscopic analysis
Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT2 cells assessed as inhibition of virus-induced giant cell formation after 4 to 5 days by microscopic analysis
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[PMID: 24686012] |
| MT2 | EC50 |
5 nM
Compound: Tenofovir alafenamide
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Antiviral activity against HIV1 3B infected in human MT2 cells assessed as protection against virus-induced cytopathic effect after 5 days by XTT assay
Antiviral activity against HIV1 3B infected in human MT2 cells assessed as protection against virus-induced cytopathic effect after 5 days by XTT assay
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[PMID: 27748590] |
| PBMC | CC50 |
1.32 μM
Compound: TAF
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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
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[PMID: 28682067] |
Tenofovir alafenamide (GS-7340) 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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 379270-37-8
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Appearance Solid
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Peso molecular 476.47
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Fòrmula C21H29N6O5P
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Color White to off-white
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SMILES
NC1=NC=NC2=C1N=CN2C[C@@H](C)OC[P@](OC3=CC=CC=C3)(N[C@@H](C)C(OC(C)C)=O)=O
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Synonyms
GS-7340
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
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 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 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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Solvente y solubilidad
DMSO : ≥ 31 mg/mL (65.06 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 6.67 mg/mL (14.00 mM; Need ultrasonic)
* "≥" means soluble, but saturation unknown.
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.
* 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, 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.
* 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)
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: ≥ 2.08 mg/mL (4.37 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.37 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.
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: 40 mg/mL (83.95 mM); Clear solution; Need ultrasonic
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureza y Documentación
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Ficha de datos (277 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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Instrucciones de manejo (2659 KB)
Referencias
[1]. Babusis D, et al. Mechanism for effective lymphoid cell and tissue loading following oral administration of nucleotide prodrug GS-7340. Mol Pharm. 2013 Feb 4;10(2):459-66. [Content Brief]
[2]. Ruane PJ, et al. Antiviral activity, safety, and pharmacokinetics/pharmacodynamics of tenofovir alafenamide as 10-day monotherapy in HIV-1-positive adults. J Acquir Immune Defic Syndr. 2013 Aug 1;63(4):449-55. [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, 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 |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.0988 mL | 10.4938 mL | 20.9877 mL | 52.4692 mL |
| 5 mM | 0.4198 mL | 2.0988 mL | 4.1975 mL | 10.4938 mL | |
| 10 mM | 0.2099 mL | 1.0494 mL | 2.0988 mL | 5.2469 mL | |
| DMSO | 15 mM | 0.1399 mL | 0.6996 mL | 1.3992 mL | 3.4979 mL |
| 20 mM | 0.1049 mL | 0.5247 mL | 1.0494 mL | 2.6235 mL | |
| 25 mM | 0.0840 mL | 0.4198 mL | 0.8395 mL | 2.0988 mL | |
| 30 mM | 0.0700 mL | 0.3498 mL | 0.6996 mL | 1.7490 mL | |
| 40 mM | 0.0525 mL | 0.2623 mL | 0.5247 mL | 1.3117 mL | |
| 50 mM | 0.0420 mL | 0.2099 mL | 0.4198 mL | 1.0494 mL | |
| 60 mM | 0.0350 mL | 0.1749 mL | 0.3498 mL | 0.8745 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.
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