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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 Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 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 |
| 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]. |
| Synonyms | S/GSK1265744 sodium, GSK-1265744 sodium, GSK1265744 sodium |
| Molecular Weight | 427.34 |
| Formula | C19H16F2N3NaO5 |
| 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 | keep 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
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Dissolve 2 mg of the compound in 100 μL DMSO
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.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
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 ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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