Dolutegravir Sodium

Catalog No.S4642 Synonyms: GSK-1349572A

For research use only.

Dolutegravir Sodium (GSK-1349572A) is a HIV integrase inhibitor with IC50 of 2.7 nM.

Dolutegravir Sodium Chemical Structure

CAS No. 1051375-19-9

Selleck's Dolutegravir Sodium has been cited by 7 Publications

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Purity & Quality Control

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Biological Activity

Description Dolutegravir Sodium (GSK-1349572A) 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 (from reference)

Cell Research:[1]
  • 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.
Animal Research:[2]
  • Animal Models: male Crl:CD (SD) rats, cynomolgus monkeys,
  • 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

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 441.36
Formula

C20H19F2N3O5.Na

CAS No. 1051375-19-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1CCOC2N1C(=O)C3=C(C(=O)C(=CN3C2)C(=O)NCC4=C(C=C(C=C4)F)F)[O-].[Na+]

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

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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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