Bictegravir
Based on 17 publication(s) in Google Scholar
Bictegravir (GS-9883) is a potent inhibitor of HIV-1 integrase with an IC50 of 7.5 nM.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.93%
- No. CAS: 1611493-60-7
- Fòrmula: C21H18F3N3O5
- Peso molecular:449.38
-
Almacenamiento:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture and light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
-
Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
-
Help & FAQs
-
NMPA-Approved Drug Library
HY-L053
-
Orally Active Compound Library
HY-L061
-
FDA Approved & Pharmacopeial Drug Library
HY-L066
-
Targeted Diversity Library
HY-L099
-
EMA-Approved Drug Library
HY-L116
-
Human Metabolite Library
HY-L123
-
Metabolic Enzyme Compound Library
HY-L146
-
Multi-Target Compound Library
HY-L176
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Drug Repurposing Compound Library Plus
HY-L035P
-
FDA-Approved Drug Library Plus
HY-L022P
-
FDA-Approved Drug Library Mini
HY-L022M
-
Bioactive Compound Library
HY-L001
-
High-Throughput Bioactive Compound Library
HY-L205
-
Mass Spectrometry Human Metabolite Library
HY-L215
-
Classic FDA-Approved Drug Library
HY-L261
-
Anti-Infection Compound Library
HY-L002
-
Metabolism/Protease Compound Library
HY-L012
-
FDA-Approved Drug Library
HY-L022
-
Antiviral Compound Library
HY-L027
-
Drug Repurposing Compound Library
HY-L035
Publications Citing Use of MedChemExpress (MCE) Bictegravir
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 Dec: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.
Actividad biológica
|
HIV-1 |
Bictegravir (BIC) inhibits the strand transfer activity with an IC50 of 7.5± 0.3 nM. Relative to its inhibition of strand transfer activity, Bictegravir is a much weaker inhibitor of 3′-processing activity of HIV-1 IN, with an IC50 of 241±51 nM. Bictegravir enhances the accumulation of 2-LTR circles ~5-fold relative to the mock-treated control and reduces the amount of authentic integration products in infected cells by 100-fold. Bictegravir potently inhibits HIV-1 replication in both MT-2 and MT-4 cells with EC50s of 1.5 and 2.4 nM, respectively. Bictegravir exhibits potent antiviral effects in both primary CD4+ T lymphocytes and monocyte-derived macrophages, with EC50s of 1.5±0.3 nM and 6.6±4.1 nM, respectively, which are comparable to values obtained in T-cell lines[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
No. CAS 1611493-60-7
-
Appearance Solid
-
Peso molecular 449.38
-
Fòrmula C21H18F3N3O5
-
Color White to light yellow
-
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
-
Synonyms
GS-9883
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture and light)
Publications (17)
-
Journal Impact Factor
-
Most Recent
-
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 -
-
Biomed Pharmacother
Differential adipose tissue remodeling and metabolic effects of dolutegravir and bictegravir: implications for HIV therapy. [Abstract]2025 Dec:193:118831. PMID: 41317481 -
-
-
-
-
Solvente y solubilidad
DMSO : 100 mg/mL (222.53 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, 1 year; -20°C, 6 months (sealed storage, away from moisture and light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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, 1 year; -20°C, 6 months (sealed storage, away from moisture and light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.56 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.56 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal 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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture and light)
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.
Protocolo
MT-2 cells are infected in bulk culture with HIV-1 IIIb at a cell density of 2×106 cells/mL for 3 h at 37°C. Infected MT-2 cells receive either DMSO (mock-treated control) or Bictegravir (BIC) at a final concentration greater than or equal to 20 times their respective antiviral 50% effective concentration (EC50). These plates are incubated at 37°C for either 12 h (for late reverse transcription product quantification) or 24 h (for 2-LTR circle and Alu-LTR product quantification), after which time the cells are harvested for total DNA isolation. DNA is extracted from each well using the DNA minikit and collected as a 100-μL eluate. TaqMan real-time PCR-quantified 2-LTR junctions (2-LTR circles), late reverse transcription products, and integration junctions (Alu-LTR) are normalized to the level of host globin gene in each sample[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
-
Ficha de datos (275 KB)
-
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
-
Instrucciones de manejo (2659 KB)
Referencias
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, 1 year; -20°C, 6 months (sealed storage, away from moisture and light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2253 mL | 11.1264 mL | 22.2529 mL | 55.6322 mL |
| 5 mM | 0.4451 mL | 2.2253 mL | 4.4506 mL | 11.1264 mL | |
| 10 mM | 0.2225 mL | 1.1126 mL | 2.2253 mL | 5.5632 mL | |
| 15 mM | 0.1484 mL | 0.7418 mL | 1.4835 mL | 3.7088 mL | |
| 20 mM | 0.1113 mL | 0.5563 mL | 1.1126 mL | 2.7816 mL | |
| 25 mM | 0.0890 mL | 0.4451 mL | 0.8901 mL | 2.2253 mL | |
| 30 mM | 0.0742 mL | 0.3709 mL | 0.7418 mL | 1.8544 mL | |
| 40 mM | 0.0556 mL | 0.2782 mL | 0.5563 mL | 1.3908 mL | |
| 50 mM | 0.0445 mL | 0.2225 mL | 0.4451 mL | 1.1126 mL | |
| 60 mM | 0.0371 mL | 0.1854 mL | 0.3709 mL | 0.9272 mL | |
| 80 mM | 0.0278 mL | 0.1391 mL | 0.2782 mL | 0.6954 mL | |
| 100 mM | 0.0223 mL | 0.1113 mL | 0.2225 mL | 0.5563 mL |
Bictegravir Related Classifications
HY-17605 Related Classifications
Powered by Bioz