Cabotegravir sodium
Based on 14 publication(s) in Google Scholar
Cabotegravir (GSK-1265744) sodium 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 sodium is primarily metabolized by uridine diphosphate glucuronosyltransferase (UGT) 1A1, with low potential to interact with other antiretroviral agents (ARVs). Cabotegravir sodium can be used to research AIDS.
For research use only. We do not sell to patients.
- Purity: 99.87%
- CAS No.: 1051375-13-3
- Formula: C19H16F2N3NaO5
- Molecular Weight:427.33
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications Citing Use of MedChemExpress (MCE) Cabotegravir sodium
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.
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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
Biological Activity
IC50: 2.5 nM (HIVADA)[1]
IC50: 0.41 μM (OAT3), 0.81 μM (OAT1)[2]
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1051375-13-3
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Appearance Solid
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Molecular Weight 427.33
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Formula C19H16F2N3NaO5
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Color White to off-white
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SMILES
FC1=C(CNC(C2=CN3C(C(N([C@@H](C)CO4)[C@@]4([H])C3)=O)=C(O[Na])C2=O)=O)C=CC(F)=C1
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Synonyms
GSK-1265744 sodium; S/GSK1265744 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
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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 sodium 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 sodium 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 sodium 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 sodium 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 sodium 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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Solvent & Solubility
DMSO : 6.25 mg/mL (14.63 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (278 KB)
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SDS (398 KB)
- English - EN (398 KB)
- Français - FR (398 KB)
- Deutsch - DE (398 KB)
- Norwegian - NO (398 KB)
- Español - ES (398 KB)
- Swedish - SV (398 KB)
- Italian - IT (398 KB)
- Korean - KR (398 KB)
- Portuguese - PT (398 KB)
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Handling Instructions (2659 KB)
References
[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. 2016;46(5):445-56. [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, 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 | 2.3401 mL | 11.7006 mL | 23.4011 mL | 58.5028 mL |
| 5 mM | 0.4680 mL | 2.3401 mL | 4.6802 mL | 11.7006 mL | |
| 10 mM | 0.2340 mL | 1.1701 mL | 2.3401 mL | 5.8503 mL |