For research use only.
Catalog No.S2667 Synonyms: S/GSK1349572
CAS No. 1051375-16-6
Dolutegravir (GSK1349572, S/GSK1349572) is a two-metal-binding HIV integrase inhibitor with IC50 of 2.7 nM in a cell-free assay, modest activity against raltegravir-resistant signature mutants Y143R, Q148K, N155H, and G140S/Q148H.
Selleck's Dolutegravir (GSK1349572) has been cited by 19 publications
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|Description||Dolutegravir (GSK1349572, S/GSK1349572) is a two-metal-binding HIV integrase inhibitor with IC50 of 2.7 nM in a cell-free assay, modest activity against raltegravir-resistant signature mutants Y143R, Q148K, N155H, and G140S/Q148H.|
|Features||A next-generation and two-metal-binding HIV integrase strand transfer inhibitor.|
S/GSK1349572 shows the potent inhibitory effect on nine clinical isolates from integrase inhibitor-naive HIV-2-infected patients with EC50 ranging from 0.2 nM -1.4 nM.  In vitro, S/GSK1349572 inhibits recombinant HIV-1 integrase-catalyzed strand transfer with IC50 of 2.7 nM. Furthermore, S/GSK1349572 potently inhibits HIV replication in cells such as peripheral blood mononuclear cells (PBMCs), MT-4 cells and CIP4 cells infected with a self-inactivating PHIV lentiviral vector with EC50 of 0,51 nM, 0.71 nM and 2.2 nM, respectively.  In vitro, S/GSK1349572 exhibits potent activity against five different nonnucleoside reverse transcription inhibitor--resistant or nucleoside reverse transcription inhibitor--resistant viruses with EC50 ranging from 1.3 nM -2.1 nM. Similarly to that against wild-type virus, S/GSK1349572 shows equivalent activity against two protease inhibitor-resistant viruses with EC50 of 0.36 nM and 0.37 nM, respectively. 
In vitro strand transfer assay:The inhibitory potencies of S/GSK1349572 and other INIs are measured in a strand transfer assay using recombinant HIV integrase. A complex of integrase and biotinylated preprocessed donor DNA-streptavidin-coated Acintillation proximity assay (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 morpholinepropanesulfonic acid (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 INIs for 60 minutes at 37 °C. Then a 3H-labeled target DNA substrate is added to give a final concentration of 7 nM substrate, and the strand transfer reaction mixture is incubated at 37 °C for 25 to 45 minutes, which allows for a linear increase in the strand transfer of donor DNA to radiolabeled target DNA. The signal is read using a Wallac MicroBeta scintillation plate reader.
|In vitro||DMSO||83 mg/mL warmed (197.91 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04166474||Not yet recruiting||Drug: Dolutegravir||Hiv|Tuberculosis||Helen Reynolds|Infectious Disease Institute Kampala Uganda|Desmond Tutu HIV Centre|University of Liverpool||April 2021||Phase 4|
|NCT04771754||Not yet recruiting||Drug: Dolutegravir||HIV-1-infection||Chelsea and Westminster NHS Foundation Trust||February 19 2021||Phase 1|
|NCT04133012||Recruiting||Other: Samplings||HIV-1 Infection||ANRS Emerging Infectious Diseases|ViiV Healthcare||February 10 2020||Not Applicable|
|NCT03851588||Recruiting||Other: Placebo|Drug: Dolutegravir 50 mg||HIV Infections|Tuberculosis||University of Cape Town|Wellcome Trust|Medecins Sans Frontieres Netherlands||December 19 2019||Phase 2|
|NCT04034862||Not yet recruiting||Drug: Treatment simplification (dolutegravir lamivudine)||HIV Infections||University of Liege||October 1 2019||Phase 3|
|NCT03991013||Recruiting||Drug: Dolutegravir 50 mg|Drug: Placebo||HIV Infections||University of Cape Town|Wellcome Trust|Médecins Sans Frontières Belgium||August 8 2019||Phase 2|
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.
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