Dolutegravir Sodium

Catalog No.S4642 Synonyms: GSK-1349572A

Dolutegravir Sodium Chemical Structure

Molecular Weight(MW): 441.36

Dolutegravir sodium is a HIV integrase inhibitor with IC50 of 2.7 nM.

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  • Comparison of the activity of dolutegravir (DTG), raltegravir (RAL), and elvitegravir (EVG) against wild-type HIV-2ROD9. Values for RAL and EVG include data from two previously-published studies of HIV-2 from our group [14,15] plus additional determinations; all data were obtained using the single-cycle assay. Bars indicate mean 50% effective concentrations (EC50); the number of independent determinations (n) for each strain is shown below the x-axis. P values were obtained via analysis of variance (ANOVA) of log10-transformed EC50 values with Tukey’s post test (Prism v6.0). No cytotoxic effects were observed in dolutegravir-treated MAGIC-5A cultures at concentrations as high as 10,000 nM.

    Retrovirology, 2015, 12:10. Dolutegravir Sodium purchased from Selleck.

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Biological Activity

Description Dolutegravir sodium is a HIV integrase inhibitor with IC50 of 2.7 nM.
Targets
HIV integrase [1]
(Cell-free assay)
2.7 nM
In vitro

Dolutegravir(S/GSK1349572) inhibits HIV-1 integrase-catalyzed strand transfer with a 50% inhibitory concentration (IC50) of 2.7 nM. S/GSK1349572 inhibits both the HIV integration reaction strand transfer step in vitro and HIV replication in cells with similar potencies. The inhibitor has no effect on total viral DNA synthesis in infected cells but blocks the integration of viral DNA into host DNA with the same potency as its antiviral effect[1].

In vivo The bioavailability of dolutegravir was high when administered as a solution, but was limited by dissolution rate or solubility when administered as a suspension. Dolutegravir is the major circulating component in mice, rats, and monkeys, with direct ether glucuronidation shown to be the primary biotransformation pathway. Dolutegravir is primarily eliminated via the feces either unabsorbed or by hydrolysis of the glucuronide or glucose conjugate[2].

Protocol

Cell Research:[1]
+ Expand
  • Cell lines: MT-4 cells
  • Concentrations: 0.16, 0.8, 4, 20 nM
  • Incubation Time: 6 h or 18 h
  • Method: In vitro growth inhibition (cytotoxicity) studies are conducted with S/GSK1349572 in proliferating human leukemic and lymphomic cell lines (IM-9, U-937, MT-4, and Molt-4) as well as in stimulated and unstimulated human PBMCs. ATP levels are quantified by using the CellTiter-Glo luciferase reagent to measure the ability of a compound to inhibit cell growth as an indicator of the compound's potential for cytotoxicity.
    (Only for Reference)
Animal Research:[2]
+ Expand
  • Animal Models: male Crl:CD (SD) rats, cynomolgus monkeys,
  • Formulation: Formulated as a solution in N,N-dimethylacetamide and diluted with 50 Mm N-methylglucamine in 3% mannitol
  • Dosages: 5 mg/kg for i.v.; 5, 50, 100, and 250 mg/kg(rats, oral); 3, 10, and 50 mg/kg(monkeys, oral)
  • Administration: i.v./oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 0.2 mg/mL (0.45 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 441.36
Formula

C20H19F2N3O5.Na

CAS No. 1051375-19-9
Storage powder
in solvent
Synonyms GSK-1349572A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Integrase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID