Home Microbiology Integrase inhibitor Dolutegravir Sodium For research use only.

Dolutegravir Sodium

Synonyms: GSK-1349572A

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

Dolutegravir Sodium Chemical Structure

Dolutegravir Sodium Chemical Structure

CAS No. 1051375-19-9

Purity & Quality Control

Dolutegravir Sodium Related Products

Signaling Pathway

Integrase Signaling Pathways

Integrase Signaling Pathway

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
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].
Cell Research 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.
In Vivo
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].
Animal Research 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

Chemical Information & Solubility

Molecular Weight 441.36 Formula

C20H19F2N3O5.Na
CAS No. 1051375-19-9 SDF Download Dolutegravir Sodium SDF
Smiles CC1CCOC2N1C(=O)C3=C(C(=O)C(=CN3C2)C(=O)NCC4=C(C=C(C=C4)F)F)[O-].[Na+]
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 5 mg/mL ( (11.32 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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.

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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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