Cabotegravir
Based on 14 publication(s) in Google Scholar
Cabotegravir (GSK-1265744) is a orally active and long-acting HIV integrase strand transfer inhibitor and organic anion transporter 1/3 (OAT1/OAT3) inhibitor with IC50 values of 2.5 nM, 0.41 μM and 0.81 μM for HIVADA, OAT3 and OAT1, respectively. Cabotegravir is primarily metabolized by uridine diphosphate glucuronosyltransferase (UGT) 1A1, with low potential to interact with other antiretroviral agents (ARVs). Cabotegravir can be used to research AIDS.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.92%
- CAS No.: 1051375-10-0
- Formule: C19H17F2N3O5
- Masse moléculaire:405.35
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Publications Citing Use of MedChemExpress (MCE) Cabotegravir
More- Sci Adv. 2023 Jul 14;9(28):eadg2955. [Abstract]
- Pharmaceutics. 2022 Aug 24;14(9):1761. [Abstract]
- Int J Antimicrob Agents. 2019 Dec;54(6):814-819. [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]
- Toxicol Appl Pharmacol. 2025 May 4:500:117371. [Abstract]
- Drug Metab Dispos. 2019 May;47(5):535-544. [Abstract]
- J Chromatogr B Analyt Technol Biomed Life Sci. 2025 Dec 15:1267:124803. [Abstract]
- University of Debrecen. 2023.
- Preprints. 2024 Apr 23.
- University of British Columbia. 2024 Apr 18.
Customer Validation & Images
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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Flow Cytometry
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Flow Cytometry
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Cell Proliferation/Viability Assay
Activité biologique
IC50: 2.5 nM (HIVADA)[1]
IC50: 0.41 μM (OAT3), 0.81 μM (OAT1)[2]
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Cell Line
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Type | Value | Description | References |
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| HEK-293T | IC50 |
0.5 nM
Compound: 4, S/GSK1265744, S/GSK744
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Antiviral activity against pseudo Human immunodeficiency virus infected in HEK293T cells after 2 days
Antiviral activity against pseudo Human immunodeficiency virus infected in HEK293T cells after 2 days
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[PMID: 23845180] |
| HEK-293T | IC50 |
30 nM
Compound: 4, S/GSK1265744, S/GSK744
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Antiviral activity against pseudo Human immunodeficiency virus infected in HEK293T cells after 2 days in presence of human serum albumin
Antiviral activity against pseudo Human immunodeficiency virus infected in HEK293T cells after 2 days in presence of human serum albumin
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[PMID: 23845180] |
| MT4 | IC50 |
1.3 nM
Compound: 4, S/GSK1265744, S/GSK744
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Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT4 cells after 4 to 5 days by bioluminescence assay
Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT4 cells after 4 to 5 days by bioluminescence assay
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[PMID: 23845180] |
Cabotegravir (GSK-1265744) inhibits the HIV-1 integrase catalyzed strand transfer reaction with an IC50 of 3.0 nM in vitro. The antiviral EC50 against HIV-1 Ba-L is 0.22 nM and that against NL432 is 0.34 nM in PBMCs, 0.57 nM using CellTiter-Glo and 1.3 nM using MTT in MT-4, and 0.5 nM in the PHIV assay, which uses a pseudotyped self-inactivating virus[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MT-4 cells
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Concentration:0-32 nM
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Incubation Time:4 or 5 days
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Result:Showed antiviral activity with an EC50 of 1.3 nM.
Chemical Information
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CAS No. 1051375-10-0
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Appearance Solid
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Masse moléculaire 405.35
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Formule C19H17F2N3O5
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Color White to yellow
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SMILES
FC1=C(CNC(C2=CN3C(C(N([C@@H](C)CO4)[C@@]4([H])C3)=O)=C(O)C2=O)=O)C=CC(F)=C1
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Synonyms
GSK-1265744; S/GSK1265744
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (14)
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Journal Impact Factor
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Most Recent
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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 -
Int J Antimicrob Agents
2019 Dec;54(6):814-819. PMID: 31479744 -
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
Cabotegravir purchased from MedChemExpress. Usage Cited in: J Infect Dis. 2025 Jul 15:jiaf362. [Abstract]
Cabotegravir (CAB, 5.0mg/kg, administered via oral gavage daily). The viability rate is depicted.
Cabotegravir purchased from MedChemExpress. Usage Cited in: J Infect Dis. 2025 Jul 15:jiaf362. [Abstract]
Cabotegravir (CAB, 5.0mg/kg, administered via oral gavage daily). Dam litter size and percent increase in maternal weight normalized to litter size.
Cabotegravir purchased from MedChemExpress. Usage Cited in: J Infect Dis. 2025 Jul 15:jiaf362. [Abstract]
Cabotegravir (CAB, 5.0 mg/kg, gavage once daily). Representative SSEA3 + flow plot of DTG dose response in CA1S hESCs compared with the fluorescence minus 1 (FMO) and 0.1% DMSO controls; vertical line denotes SSEA-3 positivity.
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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
Cabotegravir purchased from MedChemExpress. Usage Cited in: J Infect Dis. 2022 Nov 28;226(11):1992-2001. [Abstract]
Exposure to bictegravir (BIC)-, Cabotegravir (CAB, 5.0 mg/kg, gavage once daily)-, and dolutegravir (DTG)-containing combination antiretroviral therapy (cART) results in loss of pluripotency markers. SSEA-3+ and TRA-1-60+ expression normalized to corresponding 0.1% dimethyl sulfoxide (DMSO) vehicle controls (dashed lines), after exposure to no treatment (culture media without 0.1% DMSO, Ø), or 1× Cmax (unless indicated) cART regimens, in CA1S (left, n = 5) and H9 (right, n = 6, with an additional n = 4 at 0.5× Cmax) cells, respectively. Data collected via flow cytometry.
Cabotegravir purchased from MedChemExpress. Usage Cited in: J Infect Dis. 2022 Nov 28;226(11):1992-2001. [Abstract]
Bictegravir (BIC), Cabotegravir (CAB, 5.0 mg/kg, gavage once daily), and dolutegravir (DTG) human embryonic stem cell (hESC) toxicity and differentiation occur in a dose-dependent manner. Live cell count, viability, apoptosis normalized to 0.1% dimethyl sulfoxide (DMSO) control in CA1S (left, n = 3) and H9 (right, n = 6) hESCs treated with 5 (4 in H9) different integrase strand transfer inhibitors at various doses for 3.5 days.
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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 -
Toxicol Appl Pharmacol
2025 May 4:500:117371. PMID: 40328338 -
Drug Metab Dispos
Mechanistic Assessment of Extrahepatic Contributions to Glucuronidation of Integrase Strand Transfer Inhibitors. [Abstract]2019 May;47(5):535-544. PMID: 30804050 -
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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Solvant et solubilité
DMSO : 14 mg/mL (34.54 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, 1 year; -20°C, 6 months. 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. 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.
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.
Pureté et documentation
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Fiche technique (278 KB)
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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)
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Instruction de manipulation (2659 KB)
Références
[1]. Zhou T, et al. Creation of a nanoformulated cabotegravir prodrug with improved antiretroviral profiles. Biomaterials. 2018 Jan;151:53-65. [Content Brief]
[2]. Reese MJ, et al. Drug interaction profile of the HIV integrase inhibitor cabotegravir: assessment from in vitro studies and a clinical investigation with midazolam. Xenobiotica. 2015 Sep 4:1-12. [Content Brief]
[3]. Yoshinaga T, et al. Antiviral characteristics of GSK1265744, an HIV integrase inhibitor dosed orally or by long-acting injection. Antimicrob Agents Chemother. 2015 Jan;59(1):397-406. [Content Brief]
[4]. Andrews CD, et al. Cabotegravir long acting injection protects macaques against intravenous challenge with SIVmac251. AIDS. 2017 Feb 20;31(4):461-467. [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, 1 year; -20°C, 6 months. 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 |
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| DMSO | 1 mM | 2.4670 mL | 12.3350 mL | 24.6700 mL | 61.6751 mL |
| 5 mM | 0.4934 mL | 2.4670 mL | 4.9340 mL | 12.3350 mL | |
| 10 mM | 0.2467 mL | 1.2335 mL | 2.4670 mL | 6.1675 mL | |
| 15 mM | 0.1645 mL | 0.8223 mL | 1.6447 mL | 4.1117 mL | |
| 20 mM | 0.1234 mL | 0.6168 mL | 1.2335 mL | 3.0838 mL | |
| 25 mM | 0.0987 mL | 0.4934 mL | 0.9868 mL | 2.4670 mL | |
| 30 mM | 0.0822 mL | 0.4112 mL | 0.8223 mL | 2.0558 mL |
Cabotegravir Related Classifications
HY-15592 Related Classifications
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