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Cabotegravir sodium

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Catalog No. T62328Cas No. 1051375-13-3
Alias S/GSK1265744 sodium, GSK-1265744 sodium, GSK1265744 sodium

Cabotegravir sodium (GSK-1265744) is an orally active, membrane-permeable HIV integrase inhibitor (IC₅₀ = 2.5 μM) and also an OAT1/OAT3 inhibitor (IC₅₀ = 0.81/0.41 μM). It inhibits HIV replication and may be used in AIDS research.

Cabotegravir sodium

Cabotegravir sodium

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Purity: 99.63%
Catalog No. T62328Alias S/GSK1265744 sodium, GSK-1265744 sodium, GSK1265744 sodiumCas No. 1051375-13-3
Cabotegravir sodium (GSK-1265744) is an orally active, membrane-permeable HIV integrase inhibitor (IC₅₀ = 2.5 μM) and also an OAT1/OAT3 inhibitor (IC₅₀ = 0.81/0.41 μM). It inhibits HIV replication and may be used in AIDS research.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
10 mg$41-In Stock
25 mg$64-In Stock
50 mg$91-In Stock
100 mg$129-In Stock
1 mL x 10 mM (in DMSO)$30-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:99.63%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
Cabotegravir sodium (GSK-1265744) is an orally active, membrane-permeable HIV integrase inhibitor (IC₅₀ = 2.5 μM) and also an OAT1/OAT3 inhibitor (IC₅₀ = 0.81/0.41 μM). It inhibits HIV replication and may be used in AIDS research.
Targets&IC50
OAT1:0.81 μM, HIV (ADA):2.5 nM, OAT3:0.41 μM
In vitro
In vitro experiments demonstrated that Cabotegravir sodium inhibits the strand transfer reaction catalyzed by HIV-1 integrase, with a half-maximal inhibitory concentration (IC₅₀) of 3.0 nM. In PBMCs (peripheral blood mononuclear cells), the drug exhibited antiviral half-maximal effective concentrations (EC₅₀) of 0.22 nM against the HIV-1 Ba-L strain and 0.34 nM against the NL432 strain. In MT-4 cells, EC₅₀ values were determined as 0.57 nM by the CellTiter-Glo method and 1.3 nM by the MTT method, while the EC₅₀ measured in the pseudotyped self-inactivating virus PHIV assay was 0.5 nM [3].
In vivo
The half-life of Cabotegravir sodium in mice is 54 days, demonstrating a prolonged duration [1].
Cabotegravir (25 or 50 mg/kg, administered intravenously as a single or double dose) can protect Macaca mulatta (macaques) from SIVmac251 virus infection [4].
SynonymsS/GSK1265744 sodium, GSK-1265744 sodium, GSK1265744 sodium
Chemical Properties
Molecular Weight427.34
FormulaC19H16F2N3NaO5
Cas No.1051375-13-3
Smiles[Na+].C[C@H]1CO[C@@H]2Cn3cc(C(=O)NCc4ccc(F)cc4F)c(=O)c([O-])c3C(=O)N12
Storage & Solubility Information
Storagekeep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 5 mg/mL (11.7 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.3401 mL11.7003 mL23.4006 mL117.0029 mL
5 mM0.4680 mL2.3401 mL4.6801 mL23.4006 mL
10 mM0.2340 mL1.1700 mL2.3401 mL11.7003 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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