Art. -Nr.: HY-111964

Lenacapavir

(Synonyms: GS-6207)

20 Cited Publications

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Based on 20 publication(s) in Google Scholar

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.

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Reinheit: 98.44%
CAS. Nr.: 2189684-44-2
Formel: C₃₉H₃₂ClF₁₀N₇O₅S₂
Molecular Weight:968.28

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Lenacapavir Chemical Structure

CAS. Nr.: 2189684-44-2

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (20)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

HIV-1

Alle HIV Isoform-spezifische Produkte anzeigen :

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.

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

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

Chemical Information

CAS. Nr. 2189684-44-2
Appearance Solid
Molecular Weight 968.28
Formel C₃₉H₃₂ClF₁₀N₇O₅S₂
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
Synonyms

GS-6207
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (20)

All Cell Imaging/StainingCell Proliferation/Viability AssayBio/Physico-chemical Assay

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Journal Impact Factor

ACS Nano

Time-Resolved Fluorescence Imaging and Correlative Cryo-Electron Tomography to Study Structural Changes of the HIV-1 Capsid. [Abstract]

2025 Sep 2;19(34):30902-30918. PMID: 40844114

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.
Nat Commun

HIV-1 uncoating location dictates sites of integration. [Abstract]

2026 Apr 9;17(1):4840. PMID: 41957012
Nat Commun

Recurrent and novel evolutionary pathways drive in vitro HIV-1 lenacapavir resistance with diverse phenotypic consequences. [Abstract]

2026 Mar 7. PMID: 41794817

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

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

HIV-1 uncoating requires long double-stranded reverse transcription products. [Abstract]

2024 Apr 26;10(17):eadn7033. PMID: 38657061

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.
Sci Adv

Epistatic pathways can drive HIV-1 escape from integrase strand transfer inhibitors. [Abstract]

2024 Mar;10(9):eadn0042. PMID: 38427738
PLoS Pathog

HIV-1 capsid stability enables inositol phosphate-independent infection of target cells and promotes integration into genes. [Abstract]

2023 Jun 2;19(6):e1011423. PMID: 37267431
J Photochem Photobiol A Chem

2025 Nov 15;473:116930.
J Virol

Single-cell delineation of strain-specific HIV-1 Vif activities using dual reporter sensor cells and live cell imaging. [Abstract]

2025 Mar 18;99(3):e0157924. PMID: 39998123
Open Forum Infect Dis

Novel Dolutegravir and Lenacapavir Resistance Patterns in Human Immunodeficiency Virus Type 2 Infection: A Case Report. [Abstract]

2024 Nov 29;12(1):ofae705. PMID: 39741997
Viruses

Drug Interactions in Lenacapavir-Based Long-Acting Antiviral Combinations. [Abstract]

2022 May 31;14(6):1202. PMID: 35746673
Anim Cells Syst

Inducing aortic aneurysm/dissection in zebrafish: evaluating the efficacy of β-Aminopropionic Nitrile as a model. [Abstract]

2024 Mar 1;28(1):84-92. PMID: 38440122
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
bioRxiv

Damaging the conical morphology of HIV-1 capsid by targeting the FG-binding pocket and disfavoring pentameric subunits needed for core closure. [Abstract]

2026 Mar 20:2026.03.19.712970. PMID: 41889801
bioRxiv

2026 Feb 16.
Emory University

2025.
bioRxiv

The host protein cyclophilin A inhibits HIV-1 nuclear entry by decreasing capsid elasticity. [Abstract]

2025 Sep 3:2025.09.03.673798. PMID: 40950186
bioRxiv

The primary mechanism for highly potent inhibition of HIV-1 maturation by lenacapavir. [Abstract]

2024 Dec 7:2024.12.06.627250. PMID: 39677622
bioRxiv

Structural and Mechanistic Bases for Resistance of the M66I Capsid Variant to Lenacapavir. [Abstract]

2024 Nov 25:2024.11.25.625199. PMID: 39651162
Preprints

2024 Apr 23.
bioRxiv

Elasticity of the HIV-1 Core Facilitates Nuclear Entry and Infection. [Abstract]

2023 Sep 30:2023.09.29.560083. PMID: 37808653

Lösungsmittel & Löslichkeit

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)

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

1.0328 mL

5.1638 mL

10.3276 mL

5 mM

0.2066 mL

1.0328 mL

2.0655 mL

10 mM

0.1033 mL

0.5164 mL

1.0328 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, 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.

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 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:

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.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (283 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]. De Clercq E, et al. Lenacapavir: A capsid inhibitor for HIV-1 treatment and prevention. Biochem Pharmacol. 2025 Oct;240:117125. [Content Brief]

[2]. Link JO, et al. Clinical targeting of HIV capsid protein with a long-acting small molecule. Nature. 2020;584(7822):614-618. [Content Brief]

[3]. Singh K, et al. GS-CA Compounds: First-In-Class HIV-1 Capsid Inhibitors Covering Multiple Grounds. Front Microbiol. 2019;10:1227. Published 2019 Jun 20. [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

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

Keywords

Lenacapavir

20 Cited Publications

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Lenacapavir

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

Publications Citing Use of MedChemExpress (MCE) Lenacapavir

Alle HIV Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (20)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Lenacapavir

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

Publications Citing Use of MedChemExpress (MCE) Lenacapavir

Alle HIV Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (20)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Lenacapavir Related Classifications

Art. -Nr.: HY-111964