Cabotegravir (Synonyms: GSK-1265744; S/GSK1265744)

Name: Cabotegravir
Brand: MedChemExpress
SKU: HY-15592
Rating: 5.0 (14 reviews)

Art. -Nr.: HY-15592 Reinheit: 99.91%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

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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CAS. Nr. : 1051375-10-0

Größe	Verfügbarkeit	Menge
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	Auf Lager	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	Auf Lager	Estimated Time of Arrival: December 31
Solid
5 mg	Auf Lager	Estimated Time of Arrival: December 31
10 mg	Auf Lager	Estimated Time of Arrival: December 31
25 mg	Auf Lager	Estimated Time of Arrival: December 31
50 mg	Auf Lager	Estimated Time of Arrival: December 31
100 mg	Auf Lager	Estimated Time of Arrival: December 31
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This product is a controlled substance and not for sale in your territory.

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Based on 14 publication(s) in Google Scholar

Other Forms of Cabotegravir:

Dolutegravir In-stock
Cabotegravir-d₅ In-stock
Cabotegravir sodium In-stock
Cabotegravir-d₃-1 Angebot einholen
Cabotegravir-d₆ Angebot einholen
Cabotegravir (Standard) Angebot einholen

14 Publications Citing Use of MCE Cabotegravir

In Vivo Efficacy Study

Flow Cytometry

Cell Proliferation/Viability Assay

: 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.

: 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.

Spezialitätsempfehlungen

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Alle HIV Isoform-spezifische Produkte anzeigen:

Alle Isoformen anzeigen

HIV HIV-1 HIV-2

Biologische Aktivität
Reinheit & Dokumentation
Verweise
Kundenbewertung

Beschreibung

IC₅₀ & Target

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

Cellular Effect

Cell Line	Type	Value	Description	References
HEK-293T	IC₅₀	0.5 1 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	0.5 1 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]
MT4	IC₅₀	1.3 1 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]
HEK-293T	IC₅₀	30 1 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]
HEK-293T	IC₅₀	30 1 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 1 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]
HEK-293T	IC₅₀	0.5 1 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 1 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 1 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.

Molekulargewicht

405.35

Formel

C₁₉H₁₇F₂N₃O₅

CAS. Nr.

1051375-10-0

Appearance

Solid

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

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

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the 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.

Molaritätsrechner
Verdünnungsrechner

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Reinheit & Dokumentation

Purity: 99.91%

Select Batch:

Data Sheet (278 KB) SDS (394 KB)

COA (252 KB) HNMR (296 KB) LCMS (93 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]

Complete Stock Solution Preparation Table

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

Cabotegravir Related Classifications

Infection

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Cabotegravir (Synonyms: GSK-1265744; S/GSK1265744)

Kundenbewertung

Other Forms of Cabotegravir:

Cabotegravir Related Antibodies

14 Publications Citing Use of MCE Cabotegravir

Spezialitätsempfehlungen

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Alle HIV Isoform-spezifische Produkte anzeigen:

Biologische Aktivität

Reinheit & Dokumentation

Verweise

Kundenbewertung

Cabotegravir Related Antibodies

Molaritätsrechner

Verdünnungsrechner

Complete Stock Solution Preparation Table

Cabotegravir Related Classifications

Keywords:

Ihre kürzlich angesehenen Produkte:

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SAFETY DATA SHEET (SDS)

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