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Dolutegravir Sodium Integrase inhibitor

Cat.No.S4642

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

Batch: Purity: 99.94%
99.94

Solubility

In vitro
Batch:

DMSO : 5 mg/mL (11.32 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
Batch:

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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.

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
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Chemical Information, Storage & Stability

Molecular Weight 441.36 Formula

C20H19F2N3O5.Na

Storage (From the date of receipt)
CAS No. 1051375-19-9 Download SDF Storage of Stock Solutions

Synonyms GSK-1349572A SMILES CC1CCOC2N1C(=O)C3=C(C(=O)C(=CN3C2)C(=O)NCC4=C(C=C(C=C4)F)F)[O-].[Na+]

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Mechanism of Action

Targets/IC50/Ki
HIV integrase
(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.
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.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-08-14)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT07393659 RECRUITING
HIV Infections
ViiV Healthcare
2026-07-21 PHASE3
NCT07792096 NOT_YET_RECRUITING
HIV Infection
University College, London
2026-11 PHASE3
NCT07711223 RECRUITING
Infection, Human Immunodeficiency Virus
Jiangsu Aidea Pharmaceutical Group Co., Ltd.
2025-11-07 PHASE1; PHASE2
NCT07616739 NOT_YET_RECRUITING
HIV-1-infection
Fundación Huésped
2026-06-15 PHASE4
NCT05630638 RECRUITING
HIV
University of Liverpool
2023-10-10 PHASE4
NCT07555431 RECRUITING
HTLV-1 Infection; HTLV I Associated Myelopathies; HTLV I Associated T Cell Leukemia Lymphoma; Neuritis
Carlos Brites
2026-05-07 PHASE2

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