Bictegravir sodium
Based on 17 publication(s) in Google Scholar
Bictegravir sodium is a potent inhibitor of HIV-1 integrase, with an IC50 of 7.5 nM. Bictegravir sodium exhibits potent and selective anti-HIV activity and low cytotoxicity.
For research use only. We do not sell to patients.
- Purity: 99.62%
- CAS No.: 1807988-02-8
- Formula: C21H17F3N3NaO5
- Molecular Weight:471.36
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Storage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Bictegravir sodium
More- Science. 2020 Feb 14;367(6479):806-810. [Abstract]
- Sci Adv. 2023 Jul 14;9(28):eadg2955. [Abstract]
- Pharmaceutics. 2022 Aug 24;14(9):1761. [Abstract]
- Antiviral Res. 2025 Sep 11:106283. [Abstract]
- Antimicrob Agents Chemother. 2019 Dec 20;64(1):e01717-19. [Abstract]
- J Infect Dis. 2025 Jul 15:jiaf362. [Abstract]
- J Infect Dis. 2022 Nov 28;226(11):1992-2001. [Abstract]
- Open Forum Infect Dis. 2024 Nov 29;12(1):ofae705. [Abstract]
- Viruses. 2024 Oct 13;16(10):1607. [Abstract]
- J Chromatogr B Analyt Technol Biomed Life Sci. 2025 Dec 15:1267:124803. [Abstract]
- University of Debrecen. 2023.
- Biomed Pharmacother. 2025 Nov 28:193:118831. [Abstract]
- Preprints. 2024 Apr 23.
- Preprints. 2024 Apr 19.
- University of British Columbia. 2024 Apr 18.
- Charles University. 2020 Jun.
- bioRxiv. 2020 May.
Biological Activity
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HIV-1 |
Bictegravir sodium potently inhibits HIV-1 replication in both MT-2 and MT-4 cells with EC50s of 1.5 and 2.4 nM, respectively, and selectivity indices (50% cytotoxic concentration [CC50]/EC50) of ～6,800 in MT-2 cells and ～1,500 in MT-4 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1807988-02-8
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Appearance Solid
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Molecular Weight 471.36
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Formula C21H17F3N3NaO5
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Color Off-white to light yellow
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SMILES
O=C1N([C@](CC2)([H])C[C@]2([H])O3)[C@@]3([H])CN(C=C(C(NCC(C(F)=CC(F)=C4)=C4F)=O)C5=O)C1=C5O[Na]
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Synonyms
GS-9883 sodium
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (17)
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Journal Impact Factor
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Most Recent
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Science
Structural basis of second-generation HIV integrase inhibitor action and viral resistance. [Abstract]2020 Feb 14;367(6479):806-810. PMID: 32001525 -
Sci Adv
GRL-142 binds to and impairs HIV-1 integrase nuclear localization signal and potently suppresses highly INSTI-resistant HIV-1 variants. [Abstract]2023 Jul 14;9(28):eadg2955. PMID: 37436982 -
Pharmaceutics
A Pharmacokinetic Dose-Optimization Study of Cabotegravir and Bictegravir in a Mouse Pregnancy Model. [Abstract]2022 Aug 24;14(9):1761. PMID: 36145509 -
Antiviral Res
Differential effects of antiretroviral HIV integrase inhibitors on vascular cell adhesion molecules. [Abstract]2025 Sep 11:106283. PMID: 40945692 -
Antimicrob Agents Chemother
Comparable In Vitro Activities of Second-Generation HIV-1 Integrase Strand Transfer Inhibitors (INSTIs) on HIV-1 Clinical Isolates with INSTI Resistance Mutations. [Abstract]2019 Dec 20;64(1):e01717-19. PMID: 31611362 -
J Infect Dis
Fetal Defects in Mice Treated with Integrase Strand Transfer Inhibitors: Comparison of Dolutegravir, Raltegravir, Bictegravir and Cabotegravir. [Abstract]2025 Jul 15:jiaf362. PMID: 40662735 -
J Infect Dis
Second-generation HIV integrase inhibitors induce differentiation dysregulation and exert toxic effects in human embryonic stem cell and mouse models. [Abstract]2022 Nov 28;226(11):1992-2001. PMID: 36124861 -
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
Efficacy of Integrase Strand Transfer Inhibitors and the Capsid Inhibitor Lenacapavir against HIV-2, and Exploring the Effect of Raltegravir on the Activity of SARS-CoV-2. [Abstract]2024 Oct 13;16(10):1607. PMID: 39459940 -
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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Biomed Pharmacother
Differential adipose tissue remodeling and metabolic effects of dolutegravir and bictegravir: implications for HIV therapy. [Abstract]2025 Nov 28:193:118831. PMID: 41317481 -
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Solvent & Solubility
DMSO : 16.67 mg/mL (35.37 mM; ultrasonic and warming and heat to 60°C; 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 and light). 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 and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (273 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
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 and light). 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 | 2.1215 mL | 10.6076 mL | 21.2152 mL | 53.0380 mL |
| 5 mM | 0.4243 mL | 2.1215 mL | 4.2430 mL | 10.6076 mL | |
| 10 mM | 0.2122 mL | 1.0608 mL | 2.1215 mL | 5.3038 mL | |
| 15 mM | 0.1414 mL | 0.7072 mL | 1.4143 mL | 3.5359 mL | |
| 20 mM | 0.1061 mL | 0.5304 mL | 1.0608 mL | 2.6519 mL | |
| 25 mM | 0.0849 mL | 0.4243 mL | 0.8486 mL | 2.1215 mL | |
| 30 mM | 0.0707 mL | 0.3536 mL | 0.7072 mL | 1.7679 mL |
Bictegravir sodium Related Classifications
HY-17605A Related Classifications
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