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    Dolutegravir (GSK1349572)
    Dolutegravir (GSK1349572)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1832
    CAS #: 1051375-16-6 Purity ≥98%

    Description: Dolutegravir (formerly also known as GSK1349572, S/GSK1349572) is a novel, potent and orally bioavailable two-metal-binding HIV integrase inhibitor with IC50 of 2.7 nM in a cell-free assay. Dolutegravir is an FDA-approved drug that is used in combination with other medications for the treatment of HIV/AIDS infection. It demonstrated modest activity against raltegravir-resistant signature mutants Y143R, Q148K, N155H, and G140S/Q148H. It is used for the treatment of HIV-infected adults who have never received any HIV therapy (treatment-naïve) and HIV-infected adults who have previously taken HIV therapy (treatment-experienced).  It may also be used, as part of post exposure prophylaxis, to prevent HIV infection following potential exposure. 

    References: AIDS. 2010 Nov 13;24(17):2753-5; Antimicrob Agents Chemother. 2011 Feb;55(2):813-21. 

    Related CAS#: 1051375-19-9 (sodium); Dolutegravir intermediate-1 (1335210-23-5)

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    Molecular Weight (MW)419.38
    FormulaC20H19F2N3O5
    CAS No.1051375-16-6 (free acid); 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 83 mg/mL (197.9 mM)          
    Water:<1 mg/mL 
    Ethanol:<1 mg/mL
    SMILESO=C(C1=CN(C2=C(O)C1=O)C[[email protected]]3([H])OCC[[email protected]@H](C)N3C2=O)NCC4=CC=C(F)C=C4F
    SynonymsS/GSK1349572; GSK1349572; GSK-1349572; GSK 1349572. Tivicay; S/GSK-1349572; (4R,12aS)-N-(2,4-difluorobenzyl)-7-hydroxy-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-pyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazine-9-carboxamide


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    In Vitro

    In vitro activity: 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.


    Kinase 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.  


    Cell Assay: MT-4 cells growing exponentially at a density of 500000 or 600000 /mL are infected with HIV-1 strain IIIB at a viral multiplicity of infection of 0.001 or a 50% tissue culture infective dose of 4 to 10. The cells are then aliquoted to 96-well plates in the presence of varying concentrations of S/GSK1349572. After incubation for 4 or 5 days, antiviral activity is determined by a cell viability assay that either measured bioluminescence with a CellTiter-Glo luminescent reagent or measured absorbance at 560 and 690 nm using the yellow tetrazolium MTT reagent [3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyltetrazolium bromide]. 

    In VivoIn C57BL/6 mice, S/GSK1349572 significantly increases serum creatinine, which is consistent with integrase inhibitors competitively inhibiting creatinine secretion. 
    Animal modelC57BL/6 mice 
    Formulation & Dosage2.7 mg/kg/day; administrated orally for two weeks.
    References

    AIDS. 2010 Nov 13;24(17):2753-5; Antimicrob Agents Chemother. 2011 Feb;55(2):813-21; Antivir Chem Chemother. 2015 Apr;24(2):72-6. 


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Dolutegravir (GSK1349572)

    Effects of inhibitors on various forms of viral DNA in MT-4 cells. Antimicrob Agents Chemother. 2011 Feb;55(2):813-21. Dolutegravir (GSK1349572)
     

    Dolutegravir (GSK1349572)

    Long-term culture of infected MT-2 cells with escalating concentrations of INIs. Antimicrob Agents Chemother. 2011 Feb;55(2):813-21.


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