Dolutegravir (GSK1349572)

製品コードS2667 別名:S/GSK1349572

Dolutegravir (GSK1349572)化学構造


Dolutegravir (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.

サイズ 価格(税別)  
JPY 74700.00
JPY 44820.00
JPY 61420.00
JPY 161020.00


  • qPCR kinetics of 2-LTRc and integrated DNA forms during a single round of HIV replication in the presence of inhibitors. MT4cells were infected with HIV-1 in the absence (DMSO) or in the presence of 100 nM EFV, 500 nM RAL, 500 nM DTG, 10 μM RDS1611, 10 μM RDS1644, 10 μM RDS1823 added at the time of infection (black bar) or 16 h p.i. (grey bar). Samples were analyzed for (A) total viral DNA at 24 h and (B) 2-LTRc and (C) integrated viral DNA at 48 h. The graph represents the average and standard deviation of three independent experiments. Significant at: p value < 0.05 (*); p value < 0.01 (**); p value < 0.001 (***); p value < 0.0001 (****).

    Antiviral Res, 2016, 134:236-243. Dolutegravir (GSK1349572) purchased from Selleck.

    Comparison of the activity of dolutegravir (DTG), raltegravir (RAL), and elvitegravir (EVG) against wild-type HIV-2ROD9. The number of independent determinations (n) for each strain is shown below the x-axis. No cytotoxic effects were observed in dolutegravir-treated MAGIC-5A cultures at concentrations as high as 10,000 nM.

    Retrovirology, 2015, 10.1186/s12977-015-0146-8. Dolutegravir (GSK1349572) purchased from Selleck.

  • Strand transfer was carried out with RSV IN(1-269) (4 uM) and GU320R(2 uM)in the presence of 50mM NDSB201. Increasing concentrations of STIs were added as indicated at the top; DTG(Dolutegravir) in lanes 3-5, MK-2048 in lanes 6-8, and RAL in lanes 9-11. No STI was present in lane 2, and lane 1 contains the molecular weight markers. Strand transfer products and ODN substrate are identified on the right. CHS, circular half-site; OC target and SC target, open circular and supercoiled target DNA, respectively.

    J Biol Chem 2014 289(28), 19648-58. Dolutegravir (GSK1349572) purchased from Selleck.




製品説明 Dolutegravir (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.
特性 A next-generation and two-metal-binding HIV integrase strand transfer inhibitor.
HIV integrase [2]
(Cell-free assay)
2.7 nM

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. [1] 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. [2] 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. [2]

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MDCK2 cells MXvGeY5kfGmxbjDhd5NigQ>? M{LmVGlvcGmkaYTpc44hd2ZiaIXtZY4hV0OWMjDlfJBz\XO|ZXSgbY4hVUSFS{KgZ4VtdHNidYPpcochYzF2Q23t[ZRnd3KvaX6gZZMhe3Wkc4TyZZRmKGK7IHzpdZVq\CC|Y3nueIltdGG2aX;uJINwfW62aX7nJIFv[Wy7c3nz NEXENoQzOzF|MkOzOC=>





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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.


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  • 細胞株: MT-4
  • 濃度: 0 to 10 μM
  • 反応時間: 4 days or 5 days
  • 実験の流れ:

    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].


溶解度 (25°C)

体外 DMSO 83 mg/mL (197.91 mM) warming
Water Insoluble
Ethanol Insoluble

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。


分子量 419.38


CAS No. 1051375-16-6
in solvent
別名 S/GSK1349572





質量 (g) = 濃度 (mol/L) x 体積 (L) x 分子量 (g/mol)


  • 質量





開始濃度 x 開始体積 = 最終濃度 x 最終体積


この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1



  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):




チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2


質量 濃度 体積 分子量


NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03675815 Not yet recruiting HIV Infections Kirby Institute November 15 2018 Phase 4
NCT03602690 Recruiting HIV/AIDS French National Institute for Health and Medical Research-French National Agency for Research on AIDS and Viral Hepatitis (Inserm-ANRS) October 4 2018 Phase 2
NCT03683524 Not yet recruiting HIV-1 Infection Fundacio Lluita Contra la SIDA|ViiV Healthcare October 2018 Phase 4
NCT02882230 Not yet recruiting HIV Fondation Ophtalmologique Adolphe de Rothschild October 2018 --
NCT03706898 Recruiting HIV-1-infection|Hepatic Impairment Viriom October 1 2018 Phase 1
NCT03549689 Not yet recruiting HIV/AIDS|HIV-1-infection|Osteopenia Philip Grant|Stanford University September 1 2018 Phase 2



Handling Instructions


  • * 必須



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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID