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Cabotegravir

Catalog No. T6098   CAS 1051375-10-0
Synonyms: GSK744, GSK-1265744, S/GSK1265744

Cabotegravir (S/GSK1265744) (GSK744, GSK1265744) is a long-acting HIV integrase inhibitor and inhibits the HIV-1 integrase catalyzed strand transfer reaction (IC50: 3.0 nM).

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Cabotegravir Chemical Structure
Cabotegravir, CAS 1051375-10-0
Pack Size Availability Price/USD Quantity
10 mg In stock $ 46.00
25 mg In stock $ 89.00
50 mg In stock $ 158.00
100 mg In stock $ 198.00
1 mL * 10 mM (in DMSO) In stock $ 51.00
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Purity: 99.71%
Purity: 98.55%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Cabotegravir (S/GSK1265744) (GSK744, GSK1265744) is a long-acting HIV integrase inhibitor and inhibits the HIV-1 integrase catalyzed strand transfer reaction (IC50: 3.0 nM).
Targets&IC50 HIV-1:3.0 nM
In vivo GSK1265744 (50 mg/kg) effectively prevents high-dose SHIV infection in rhesus macaques.
Kinase Assay In vitro strand transfer assay: The inhibitory concentrations of GSK1265744 is measured in a strand transfer assay using recombinant HIV IN. A complex of integrase and biotinylated donor DNA–streptavidin-coated SPA beads is formed by incubating 2 μM purified recombinant integrase with 0.66 μM biotinylated donor DNA–4 mg/mL streptavidin-coated SPA beads in 25 mM sodium MOPS pH 7.2, 23 mM NaCl, and 10 mM MgCl2 for 5 minutes at 37°C. These beads are spun down and preincubated with diluted INSTIs for 60 minutes at 37°C. Next, [3H]-labeled target DNA substrate is added to give a final concentration of 7 nM substrate, and the strand transfer reaction is incubated at 37°C for 25 to 45 minutes, which allowed for a linear increase in strand transfer of donor DNA to radiolabeled target DNA. The signal is read using a Wallac MicroBeta scintillation plate reader.
Synonyms GSK744, GSK-1265744, S/GSK1265744
Molecular Weight 405.35
Formula C19H17F2N3O5
CAS No. 1051375-10-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 36 mg/mL (88.8 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

TargetMolReferences and Literature

1. Yoshinaga T, et al. Antimicrob Agents Chemother. 2015, 59(1), 397-406. 2. Andrews CD, et al. Sci Transl Med. 2015, 7(270), 270-274.

Related compound libraries

This product is contained In the following compound libraries:
Drug Repurposing Compound Library EMA Approved Drug Library Inhibitor Library Anti-COVID-19 Compound Library Human Metabolite Library Anti-Metabolism Disease Compound Library Bioactive Compound Library NO PAINS Compound Library Fluorochemical Library FDA-Approved & Pharmacopeia Drug Library

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Keywords

Cabotegravir 1051375-10-0 Microbiology/Virology Proteases/Proteasome HIV Protease Human immunodeficiency virus inhibit GSK744 GSK-1265744 HIV Integrase GSK-744 UGT1A1 OAT GSK 1265744 HIV S/GSK-1265744 Inhibitor S/GSK1265744 AIDS antiretroviral GSK1265744 GSK 744 S/GSK 1265744 inhibitor

 

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