1. Anti-infection
  2. HIV Reverse Transcriptase
  3. Tenofovir alafenamide hemifumarate

Tenofovir alafenamide hemifumarate  (Synonyms: GS-7340 hemifumarate)

Cat. No.: HY-15232B Purity: 99.92%
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Tenofovir alafenamide hemifumarate (GS-7340 hemifumarate) is an investigational oral proagent of Tenofovir. Tenofovir is a HIV-1 nucleotide reverse transcriptase inhibitor.

For research use only. We do not sell to patients.

CAS No. : 1392275-56-7

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO In-stock
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Customer Review

Based on 11 publication(s) in Google Scholar

Other Forms of Tenofovir alafenamide hemifumarate:

Top Publications Citing Use of Products

    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.

    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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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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

     

    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
    Molecular Weight

    534.50

    Formula

    C21H29N6O5P.1/2 C4H4O4

    CAS No.
    Appearance

    Solid

    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]

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, sealed storage, away from moisture

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

    Solvent & Solubility
    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)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.8709 mL 9.3545 mL 18.7091 mL
    5 mM 0.3742 mL 1.8709 mL 3.7418 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, 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.

    • Molarity Calculator

    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

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    Concentration (final)

    C2

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    Volume (final)

    V2

    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: ≥ 2.5 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.
    • 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.

      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.

    • 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

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: 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).
    Purity & Documentation

    Purity: 99.92%

    References

    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
    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.

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    • 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.

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    Product Name:
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