Lenacapavir
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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.44%
- CAS 番号: 2189684-44-2
- 分子式: C39H32ClF10N7O5S2
- 分子量:968.28
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 Lenacapavir
More- ACS Nano. 2025 Sep 2;19(34):30902-30918. [Abstract]
- Nat Commun. 2026 Apr 9;17(1):4840. [Abstract]
- Nat Commun. 2026 Mar 7. [Abstract]
- Sci Adv. 2024 Apr 26;10(17):eadn7033. [Abstract]
- Sci Adv. 2024 Mar;10(9):eadn0042. [Abstract]
- PLoS Pathog. 2023 Jun 2;19(6):e1011423. [Abstract]
- J Photochem Photobiol A Chem. 2025 Nov 15;473:116930.
- J Virol. 2025 Mar 18;99(3):e0157924. [Abstract]
- Open Forum Infect Dis. 2024 Nov 29;12(1):ofae705. [Abstract]
- Viruses. 2022 May 31;14(6):1202. [Abstract]
- Anim Cells Syst. 2024 Mar 1;28(1):84-92. [Abstract]
- J Chromatogr B Analyt Technol Biomed Life Sci. 2025 Dec 15:1267:124803. [Abstract]
- bioRxiv. 2026 Mar 20:2026.03.19.712970. [Abstract]
- bioRxiv. 2026 Feb 16.
- Emory University. 2025.
- bioRxiv. 2025 Sep 3:2025.09.03.673798. [Abstract]
- bioRxiv. 2024 Dec 7:2024.12.06.627250. [Abstract]
- bioRxiv. 2024 Nov 25:2024.11.25.625199. [Abstract]
- Preprints. 2024 Apr 23.
- bioRxiv. 2023 Sep 30:2023.09.29.560083. [Abstract]
Customer Validation & Images
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Cell Proliferation/Viability Assay
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Cell Imaging/Staining
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Cell Imaging/Staining
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Bio/Physico-chemical Assay
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Bio/Physico-chemical Assay
生物活性
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HIV-1 |
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Cell Line
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Type | Value | Description | References |
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| HEK-293T | CC50 |
>50 μM
Compound: 11; GS-6207
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Cytotoxicity against HEK293T cells incubated for 72 hrs by MTT assay
Cytotoxicity against HEK293T cells incubated for 72 hrs by MTT assay
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[PMID: 37393791] |
| MT4 | CC50 |
27 μM
Compound: 21
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Cytotoxicity against mouse MT4 cells
Cytotoxicity against mouse MT4 cells
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[PMID: 33751981] |
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 (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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 2189684-44-2
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性状 Solid
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分子量 968.28
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分子式 C39H32ClF10N7O5S2
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Color White to light yellow
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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
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別名
GS-6207
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (20)
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Journal Impact Factor
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Most Recent
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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.
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Nat Commun
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.
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Sci Adv
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.
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Sci Adv
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 -
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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
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 -
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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
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 -
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bioRxiv
2023 Sep 30:2023.09.29.560083. PMID: 37808653
溶剤 & 溶解度
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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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.
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.
純度とドキュメンテーション
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データシート (283 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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取扱説明書 (2659 KB)
参考文献
[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]
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 |
Lenacapavir 関連分類
HY-111964 関連分類
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