Art. -Nr.: HY-15592

Cabotegravir

(Synonyms: GSK-1265744; S/GSK1265744)

14 Cited Publications

Kundenbewertung

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 HIV_ADA, 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.

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Reinheit: 99.92%
CAS. Nr.: 1051375-10-0
Formel: C₁₉H₁₇F₂N₃O₅
Molecular Weight:405.35

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Cabotegravir Chemical Structure

CAS. Nr.: 1051375-10-0

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (14)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC₅₀: 2.5 nM (HIV_ADA)^[1]
IC₅₀: 0.41 μM (OAT3), 0.81 μM (OAT1)^[2]

Alle HIV Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK-293T	IC₅₀	0.5 nM Compound: 4, S/GSK1265744, S/GSK744	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	[PMID: 23845180]
HEK-293T	IC₅₀	30 nM Compound: 4, S/GSK1265744, S/GSK744	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	[PMID: 23845180]
MT4	IC₅₀	1.3 nM Compound: 4, S/GSK1265744, S/GSK744	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	[PMID: 23845180]

In Vitro

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.

Cell Viability Assay^[3]

Cell Line:

MT-4 cells
Concentration:

0-32 nM
Incubation Time:

4 or 5 days
Result:

Showed antiviral activity with an EC₅₀ of 1.3 nM.

In Vivo

The half-life of Cabotegravir is up to 54 days in mice^[1].
Cabotegravir (25 or 50 mg/kg; i.v.; single dose or twice) protects Macaques against intravenous challenge with SIVmac251^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 1051375-10-0
Appearance Solid
Molecular Weight 405.35
Formel C₁₉H₁₇F₂N₃O₅
Color White to yellow
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
Synonyms

GSK-1265744; S/GSK1265744
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (14)

All In Vivo Efficacy StudyFlow CytometryCell Proliferation/Viability Assay

Sort by:

Journal Impact Factor

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

Efficacy of antiretroviral compounds against Toxoplasma gondii in vitro. [Abstract]

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.
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.
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

OAT1/3 regulate the absorption of CP-25 in the rat synovium. [Abstract]

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
University of Debrecen

2023.
Preprints

2024 Apr 23.
University of British Columbia

2024 Apr 18.

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.4670 mL

12.3350 mL

24.6700 mL

5 mM

0.4934 mL

2.4670 mL

4.9340 mL

10 mM

0.2467 mL

1.2335 mL

2.4670 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 1.67 mg/mL (4.12 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during 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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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
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

Keywords

Cabotegravir

14 Cited Publications

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Cabotegravir

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Publications Citing Use of MedChemExpress (MCE) Cabotegravir

Alle HIV Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (14)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Cabotegravir

Anti-Infection Compound Library

Membrane Transporter/Ion Channel Compound Library

Metabolism/Protease Compound Library

FDA-Approved Drug Library

Antiviral Compound Library

Drug Repurposing Compound Library

Anti-COVID-19 Compound Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Pediatric Drug Library

Protein-protein Interaction Inhibitor Library

EMA-Approved Drug Library

Human Metabolite Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Classic FDA-Approved Drug Library

Publications Citing Use of MedChemExpress (MCE) Cabotegravir

Alle HIV Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (14)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Cabotegravir Related Classifications

HY-15592 Related Classifications