Lenacapavir sodium
Based on 22 publication(s) in Google Scholar
Lenacapavir (GS-6207) sodium is an HIV-1 capsid inhibitor. Lenacapavir sodium 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 sodium exhibits activity against a variety of HIV-1 subtypes and clinical isolates. Lenacapavir sodium 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 : 99.86%
- CAS 番号: 2283356-12-5
- 分子式: C39H31ClF10N7NaO5S2
- 分子量:990.26
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保管条件:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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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 sodium
More- Nat Commun. 2026 Apr 9;17(1):4840. [Abstract]
- Nat Commun. 2026 Mar 7. [Abstract]
- ACS Nano. 2025 Sep 2;19(34):30902-30918. [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 Jul 18.
- bioRxiv. 2026 Jun 25.
- 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
製品説明
体外実験
Lenacapavir sodium 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 sodium inhibits HIV-1 in MT-4 cells with a mean EC50 of 105 pM[1].
Lenacapavir sodium 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 sodium inhibits 23 HIV-1 isolates in PBMCs with a mean EC50 of 50 pM[1].
Lenacapavir sodium 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 sodium (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.
体内実験
Lenacapavir sodium (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.
化学情報
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CAS 番号 2283356-12-5
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性状 Solid
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分子量 990.26
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分子式 C39H31ClF10N7NaO5S2
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Color White to off-white
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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=C4N([Na])S(=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 sodium
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (22)
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Journal Impact Factor
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Most Recent
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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 sodium 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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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 sodium 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 sodium 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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Sci Adv
2024 Apr 26;10(17):eadn7033. PMID: 38657061
Lenacapavir sodium 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 sodium 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 -
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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
体外:
DMSO : 86.67 mg/mL (87.52 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, 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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
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.
In Vivo Dissolution Calculator
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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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 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, 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.0098 mL | 5.0492 mL | 10.0984 mL | 25.2459 mL |
| 5 mM | 0.2020 mL | 1.0098 mL | 2.0197 mL | 5.0492 mL | |
| 10 mM | 0.1010 mL | 0.5049 mL | 1.0098 mL | 2.5246 mL | |
| 15 mM | 0.0673 mL | 0.3366 mL | 0.6732 mL | 1.6831 mL | |
| 20 mM | 0.0505 mL | 0.2525 mL | 0.5049 mL | 1.2623 mL | |
| 25 mM | 0.0404 mL | 0.2020 mL | 0.4039 mL | 1.0098 mL | |
| 30 mM | 0.0337 mL | 0.1683 mL | 0.3366 mL | 0.8415 mL | |
| 40 mM | 0.0252 mL | 0.1262 mL | 0.2525 mL | 0.6311 mL | |
| 50 mM | 0.0202 mL | 0.1010 mL | 0.2020 mL | 0.5049 mL | |
| 60 mM | 0.0168 mL | 0.0842 mL | 0.1683 mL | 0.4208 mL | |
| 80 mM | 0.0126 mL | 0.0631 mL | 0.1262 mL | 0.3156 mL |
Lenacapavir sodium 関連分類
HY-111964A 関連分類
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