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  4. Lenacapavir

Lenacapavir (GS-6207) is an HIV-1 capsid inhibitor. Lenacapavir binds to the interface between capsid hexamers and CA monomers, disrupts capsid assembly and viral maturation, inhibits nuclear translocation of HIV-1 DNA, interferes with CA-mediated protein-protein interactions, reduces the formation of 2-LTR circles and pre-integration proviruses, induces aberrant capsids, and decreases the production of mature HIV-1. Lenacapavir exhibits activity against a variety of HIV-1 subtypes and clinical isolates. Lenacapavir is applicable to research related to human immunodeficiency virus type 1 (HIV-1) infection.

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

CAS No. : 2189684-44-2

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

Based on 19 publication(s) in Google Scholar

Other Forms of Lenacapavir:

Lenacapavir Related Antibodies

Top Publications Citing Use of Products

    Lenacapavir purchased from MedChemExpress. Usage Cited in: Nat Commun. 2026 Mar 7.

    Dose-dependent effects of Lenacapavir (LEN) (0.001-1 μM) on HIV-1 core stability.

    Lenacapavir purchased from MedChemExpress. Usage Cited in: ACS Nano. 2025 Sep 2;19(34):30902-30918.  [Abstract]

    Lenacapavir (LEN) (500 nM) stabilized the capsid lattice, as evidenced by a delayed/blocked CDR release from membrane-permeabilized virions (+SAP).

    Lenacapavir purchased from MedChemExpress. Usage Cited in: ACS Nano. 2025 Sep 2;19(34):30902-30918.  [Abstract]

    Lenacapavir (LEN) (500 nM) led to significantly fewer numbers of intact conically shaped capsids and a greater number of partially conical cores with compromised morphologies of HIV-1 cores, in contrast to the IP6-stabilized morphologically intact cores.

    Lenacapavir purchased from MedChemExpress. Usage Cited in: Sci Adv. 2024 Apr 26;10(17):eadn7033.  [Abstract]

    The capsid binding inhibitor Lenacapavir (LEN) (10 nM) led to the rapid (<2 hours) loss of both HIV-3.1kb and HIV-8.4kb viral DNA in aphidicolin-treated HeLa cells.

    Lenacapavir purchased from MedChemExpress. Usage Cited in: Sci Adv. 2024 Apr 26;10(17):eadn7033.  [Abstract]

    Lenacapavir (LEN) (10 nM; 10 h) led to a ～5.3- to 8.0-fold increase in the percentage of GFP reporter-expressing cells in HeLa cells infected with HIV-3.1kb.

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    Description

    Lenacapavir (GS-6207) is an HIV-1 capsid inhibitor. Lenacapavir binds to the interface between capsid hexamers and CA monomers, disrupts capsid assembly and viral maturation, inhibits nuclear translocation of HIV-1 DNA, interferes with CA-mediated protein-protein interactions, reduces the formation of 2-LTR circles and pre-integration proviruses, induces aberrant capsids, and decreases the production of mature HIV-1. Lenacapavir exhibits activity against a variety of HIV-1 subtypes and clinical isolates. Lenacapavir is applicable to research related to human immunodeficiency virus type 1 (HIV-1) infection[1][2][3].

    IC50 & Target

    HIV-1

     

    Cellular Effect
    Cell Line Type Value Description References
    HEK-293T CC50
    > 50 μM
    Compound: 11; GS-6207
    Cytotoxicity against HEK293T cells incubated for 72 hrs by MTT assay
    Cytotoxicity against HEK293T cells incubated for 72 hrs by MTT assay
    		[PMID: 37393791]
    MT4 CC50
    27 μM
    Compound: 21
    Cytotoxicity against mouse MT4 cells
    Cytotoxicity against mouse MT4 cells
    		[PMID: 33751981]
    In Vitro

    Lenacapavir inhibits HIV-1 with mean IC50 values of 200 pM in single-cycle assays and 170 pM in multicycle assays, and inhibits HIV-2 with mean IC50 values of 2.2 nM in single-cycle assays and 2.4 nM in multicycle assays[1].
    Lenacapavir inhibits HIV-1 in MT-4 cells with a mean EC50 of 105 pM[1].
    Lenacapavir inhibits HIV-1 in primary human CD4+ T cells with a mean EC50 of 32 pM and in primary human macrophages with a mean EC50 of 56 pM[1].
    Lenacapavir inhibits 23 HIV-1 isolates in PBMCs with a mean EC50 of 50 pM[1].
    Lenacapavir has its binding affinity reduced by 20-fold and viral susceptibility to it reduced by 10-fold due to the HIV-1 capsid N74D mutation[1].
    Lenacapavir (48 hours post-infection) exhibits reduced potency against HIV-1 with CA mutations associated with resistance, with fold resistance values ranging from 6-fold (Q67H) to >3226-fold (M66I) relative to wild-type HIV-1 in MT-2 cells[2].

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

    Lenacapavir Related Antibodies
    In Vivo

    Lenacapavir (subcutaneous; single dose) maintains plasma concentrations above the threshold needed for 95% HIV-1 replication inhibition for more than 12 weeks in rats[3].
    Lenacapavir (subcutaneous; single dose) maintains plasma concentrations above the threshold needed for 95% HIV-1 replication inhibition for more than 12 weeks in dogs[3].

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

    968.28

    Formula

    C39H32ClF10N7O5S2
    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    FC1=CC(F)=CC(C[C@@H](C2=NC(C#CC(S(=O)(C)=O)(C)C)=CC=C2C3=CC=C(Cl)C4=C3N(CC(F)(F)F)N=C4NS(=O)(C)=O)NC(CN5C(C(F)(F)[C@@]6([H])[C@]7([H])C6)=C7C(C(F)(F)F)=N5)=O)=C1
    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 : 200 mg/mL (206.55 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.0328 mL 5.1638 mL 10.3276 mL
    5 mM 0.2066 mL 1.0328 mL 2.0655 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.

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    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

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    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    90% Corn Oil

      Solubility: ≥ 6.25 mg/mL (6.45 mM); Clear solution

      This protocol yields a clear solution of ≥ 6.25 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 (62.5 mg/mL) to 900 μL Corn oil, and mix evenly.

    • Protocol 2

      Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: 2.5 mg/mL (2.58 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    +
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    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
    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, 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
    DMSO 1 mM 1.0328 mL 5.1638 mL 10.3276 mL 25.8190 mL
    5 mM 0.2066 mL 1.0328 mL 2.0655 mL 5.1638 mL
    10 mM 0.1033 mL 0.5164 mL 1.0328 mL 2.5819 mL
    15 mM 0.0689 mL 0.3443 mL 0.6885 mL 1.7213 mL
    20 mM 0.0516 mL 0.2582 mL 0.5164 mL 1.2909 mL
    25 mM 0.0413 mL 0.2066 mL 0.4131 mL 1.0328 mL
    30 mM 0.0344 mL 0.1721 mL 0.3443 mL 0.8606 mL
    40 mM 0.0258 mL 0.1291 mL 0.2582 mL 0.6455 mL
    50 mM 0.0207 mL 0.1033 mL 0.2066 mL 0.5164 mL
    60 mM 0.0172 mL 0.0861 mL 0.1721 mL 0.4303 mL
    80 mM 0.0129 mL 0.0645 mL 0.1291 mL 0.3227 mL
    100 mM 0.0103 mL 0.0516 mL 0.1033 mL 0.2582 mL
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    Lenacapavir 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:

    Lenacapavir2189684-44-2GS-6207GS6207GS 6207HIVHuman immunodeficiency virusCA monomersHIV-1 capsid hexamersHIV-1 DNAprimary human macrophagesMT-4 cellsprimary human CD4+ T cells2-LTR circleHIV-1 subtypesintegrated provirusHIV-1 capsid protein (CA)Inhibitorinhibitorinhibit

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