Dolutegravir (GSK1349572)

For research use only. Not for use in humans.

製品コードS2667 別名:S/GSK1349572

Dolutegravir (GSK1349572)化学構造

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.

サイズ 価格(税別)  
10mM (1mL in DMSO) JPY 76700
JPY 46800
JPY 63400
JPY 163000
最寄りの販売代理店を探す

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バルク問合せ

製品安全説明書

Integrase阻害剤の選択性比較

生物活性

製品説明 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.
特性 A next-generation and two-metal-binding HIV integrase strand transfer inhibitor.
ターゲット
HIV integrase [2]
(Cell-free assay)
2.7 nM
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MDCK2 cells MW\GeY5kfGmxbjDhd5NigQ>? MmXwTY5pcWKrdHnvckBw\iCqdX3hckBQS1R{IHX4dJJme3OnZDDpckBOTEONMjDj[YxteyC3c3nu[{BcOTSFXX3leIZwem2rbjDhd{B{fWK|dILheIUh[nlibHnxeYllKHOlaX70bYxt[XSrb36gZ492dnSrbnegZY5idHm|aYO= MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzF|MkOzOEc,OjNzM{KzN|Q9N2F-
HOS MlrZRY51cX[rcnHsJIF{e2G7 MXmzJIhzew>? M2XKWmFvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JGhKXi1zIHjhdoJwemmwZzD3bYxlKHS7cHWgbY51\We{YYPlJIlv\mWldHXkJIlvKGi3bXHuJGhQWyClZXzsd{BxemW2cnXheIVlKHerdHigZ49ueG:3bnSg[o9zKDNiaILzJIJ6KHOrbnfs[U1zd3WwZDDITXYuOSCrbn\lZ5Rqfmm2eTDhd5NigSxiRVO1NEA:KDBwMECxOkDPxE1w MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlyMU[2O{c,OjR7MEG2Olc9N2F-
HEK293T NVT4c|RuSW62aY\pdoFtKGG|c3H5 Mk\tNkBl[Xm| Mlr2RY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgdJNmfWSxIFj1cYFvKGmvbYXuc4Rm\mmlaXXuZ5khfmm{dYOgbY5n\WO2ZXSgbY4hUEWNMkmzWEBk\WyuczDh[pRmeiB{IHThfZMtKEmFNUCgQUAxNjByMUeg{txONg>? NYm4Z2RHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4OFUyQDBpPkKzPFQ2OThyPD;hQi=>
MT4 Mmm1RY51cX[rcnHsJIF{e2G7 M4rCZVQhfG9iNTDkZZl{ NVXzWIt7SW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUHWvYX6gbY1ufW6xZHXmbYNq\W6leTD2bZJ2eyBzIEPCJIlv\mWldHXkJIlvKGi3bXHuJG1VPCClZXzsd{Bi\nSncjC0JJRwKDViZHH5d{BjgSCkaX;seY1qdmW|Y3XuZ4Uh[XO|YYmsJGlEPTBiPTCwMlAxOiEQvF2u MlSxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6NEWxPFAoRjJ|OES1NVgxRC:jPh?=
HOS MkiyRY51cX[rcnHsJIF{e2G7 M1j3TFMhcHK| M2HpXGFvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JJJidHSnZ4LheolzNXKnc3nzeIFvfCCKSW[tNUBp[XKkb4LpcochcW62ZXfyZZNmKE5zNUXIJI12fGGwdDDpcoZm[3SnZDDpckBpfW2jbjDIU3Mh[2WubIOgdJJmfHKnYYTl[EB4cXSqIHPvcZBwfW6mIH\vdkA{KGi{czDifUB{cW6pbHWtdo92dmRiSFnWMVEhcW6oZXP0bZZqfHliYYPzZZktKEWFNUCgQUAxNjByM{[g{txONg>? NHvuNJQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmwNVY3Pyd-MkS5NFE3Pjd:L3G+
HOS M{Pa[mFvfGm4aYLhcEBie3OjeR?= NWTrO2dwOyCqcoO= NFfheZVCdnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEBz[Wy2ZXfyZZZqei2{ZYPpd5RidnRiSFnWMVEhcGG{Yn;ybY5oKGmwdHXndoF{\SC\MUSzVkBufXSjboSgbY5n\WO2ZXSgbY4hcHWvYX6gTG9UKGOnbHzzJJBz\XS{ZXH0[YQhf2m2aDDjc41xd3WwZDDmc5IhOyCqcoOgZpkhe2mwZ3zlMZJwfW6mIFjJWk0yKGmwZnXjeIl3cXS7IHHzd4F6NCCHQ{WwJF0hOC5yMESzJO69VS5? NWTte5hJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFE3PjdpPkK0PVAyPjZ5PD;hQi=>
HOS NGqzT4ZCdnSrdnnyZYwh[XO|YYm= NULkWGV[OyCqcoO= MUfBcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDDyZYx1\We{YY\pdk1z\XOrc4ThcpQhUEmYLUGgbIFz[m:{aX7nJIlvfGWpcnHz[UBIOTRyUz;RNVQ5UCCmb4XicIUhdXW2YX70JIlv\mWldHXkJIlvKGi3bXHuJGhQWyClZXzsd{BxemW2cnXheIVlKHerdHigZ49ueG:3bnSg[o9zKDNiaILzJIJ6KHOrbnfs[U1zd3WwZDDITXYuOSCrbn\lZ5Rqfmm2eTDhd5NigSxiRVO1NEA:KDBwMEC1PEDPxE1w MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlyMU[2O{c,OjR7MEG2Olc9N2F-
HOS NE[3OIpCdnSrdnnyZYwh[XO|YYm= MmO0N{BpenN? MX;BcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDDJUnNVUS2{ZYPpd5RidnRiSFnWMVEhcGG{Yn;ybY5oKGmwdHXndoF{\SCUMk[zT{BufXSjboSgbY5n\WO2ZXSgbY4hcHWvYX6gTG9UKGOnbHzzJJBz\XS{ZXH0[YQhf2m2aDDjc41xd3WwZDDmc5IhOyCqcoOgZpkhe2mwZ3zlMZJwfW6mIFjJWk0yKGmwZnXjeIl3cXS7IHHzd4F6NCCHQ{WwJF0hOC5yMUGg{txONg>? MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlyMU[2O{c,OjR7MEG2Olc9N2F-
HOS MkjjRY51cX[rcnHsJIF{e2G7 NETxXmw{KGi{cx?= NX;tU4xpSW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUU6VVFmtdoV{cXO2YX70JGhKXi1zIHjhdoJwemmwZzDpcpRm\3Kjc3WgS|EyQFJibYX0ZY51KGmwZnXjeIVlKGmwIHj1cYFvKEiRUzDj[YxteyCycnX0doVifGWmIIfpeIgh[2:vcH;1coQh\m:{IEOgbJJ{KGK7IIPpcodt\S2{b4Xu[EBJUVZvMTDpcoZm[3Srdnn0fUBie3OjeTygSWM2OCB;IECuNFE{KM7:TT6= M17VVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUCxOlY4Lz5{NEmwNVY3PzxxYU6=
P4R5 MAGI MlfoRY51cX[rcnHsJIF{e2G7 M4HrbFI1KGi{cx?= M3HNOmFvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JGhKXjFiaX7m[YN1\WRiaX6gR2Q1N0O[Q2K0M2NEWjViZYjwdoV{e2mwZzDoeY1idiCSNGK1JG1CT0liY3XscJMheHKnaX7jeYJifGWmIIfpeIgh[2WubIOg[o9zKDJ2IHjyd{Bnd2yub4fl[EBjgSC4aYLhcEBqdm[nY4Tpc44hdWWjc4Xy[YQh[W[2ZYKgOFghcHK|IHL5JIJmfGFvZ3HsZYN1d3OrZHHz[UBz\XCxcoTldkBo\W6nIHHzd4F6NCCHQ{WwJF0hOC5yMjFOwG0v NETFTmc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MECzNVk4Pid-M{CwN|E6PzZ:L3G+
P4R5 NVi4cYZ5SW62aY\pdoFtKGG|c3H5 NXTnN3gzOjRiaILz M4PIdWFvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JGhKXjFiaX7m[YN1\WRiaX6gR2Q1N0O[Q2K0M2NEWjViZYjwdoV{e2mwZzDoeY1idiCSNGK1JINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZidnnyZYwhemWybHnjZZRqd25icILlbY5kfWKjdHXkJJdqfGhiY3XscJMh\m:{IEK0JIhzeyCob3zsc5dm\CCkeTD2bZJidCCrbn\lZ5Rqd25ibXXhd5Vz\WRiYX\0[ZIhPDhiaILzJIJ6KGKndHGt[4Ft[WO2b4Pp[IF{\SC{ZYDvdpRmeiCpZX7lJIF{eyxiRVO1NEA:KDBwMEKg{txONg>? NUfxfHVKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki1NlUzPzlpPkK4OVI2Ojd7PD;hQi=>
HEK293T NYfLO3hHSW62aY\pdoFtKGG|c3H5 MVuyJIRigXN? NX3XSoVoSW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QheHOndXTvJGh2dWGwIHntcZVvd2SnZnnjbYVv[3lidnnyeZMhcW6oZXP0[YQhcW5iSFXLNlk{XCClZXzsd{Bi\nSncjCyJIRigXNiaX6gdJJme2WwY3Wgc4YhcHWvYX6gd4VzfW1iYXzieY1qdixiSVO1NEA:KDBwMEKyJO69VS5? MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzh2NUG4NEc,OjN6NEWxPFA9N2F-
MDCK2 NF\IUWJHfW6ldHnvckBie3OjeR?= MVTJcohq[mm2aX;uJI9nKGi3bXHuJG9EXDJiZYjwdoV{e2WmIHnuJG1FS0t{IHPlcIx{KHW|aX7nJHsyPEOfbXX0[o9zdWmwIHHzJJN2[nO2cnH0[UBjgSCuaYH1bYQhe2OrboTpcIxifGmxbjDjc5VvfGmwZzDhcoFtgXOrczygTWM2OCB;IEGuPUDPxE1w MkfjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjNzM{KzN|QoRjJ|MUOyN|M1RC:jPh?=
Vero E6 NYPk[4NwSW62aY\pdoFtKGG|c3H5 MWWyJIRigXN? MkXYRY51cX[rcnHsJIVn\mmlYXP5JIFo[Wmwc4SgV2FTWy2Fb2[tNkApe3S{YXnuJGJiflCjdEGpJIlvKF[ncn:gSVYh[2WubIOgZZN{\XO|ZXSgZpkhcW6qaXLpeIlwdiCxZjD2bZJidCCUTlGgdoVxdGmlYYTpc44hdWWjc4Xy[YQh[nliUmStVGNTKGGodHXyJFIh\GG7czygSWM2OCB;IEKyMlA1KM7:TT6= NYP2RYp[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTJ{OUKxNU8oRkOqRV3CUFww[T5?
Vero E6 MVPBcpRqfmm{YXygZZN{[Xl? NVvBOllrOiCmYYnz NV\TZnFwSW62aY\pdoFtKGWoZnnjZYN6KGGpYXnud5QhW0GUUz3Dc3YuOiBqc4TyZYlvKEKjdmDheFEqKGmwIG\ldo8hTTZiY3XscJMh[XO|ZYPz[YQh[nliaX7obYJqfGmxbjDv[kB3cXKjbDDSUmEhemWybHnjZZRqd25ibXXhd5Vz\WRiYomgVnQuWEOUIHHmeIVzKDJiZHH5d{whTUN7MDC9JFQzNjhzIN88UU4> M4HoUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFEzOjl{MUGvK|5EcEWPQly8M4E,

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アッセイ
Methods Test Index PMID
Dose-response infectivity curves
NL4.3IN(WT) / NL4.3IN(S230R) virus; 

PubMed: 29617824     


Dose-response infectivity curves in the presence of dolutegravir (DTG) for wild-type (WT) and S230R viruses. Data reflect viral resistance to DTG in TZM-bl cells. TZM-bl cells were infected with NL4.3IN(WT) or NL4.3IN(S230R) virus over 48 hours, and luciferase levels were measured. Infectivity of NL4.3IN(WT) virus is shown for comparison. Dose-response curves were produced from the compilation of 3 independent experiments, each performed in triplicate. Error bars indicate means (±standard errors of the mean). RLU, relative luminescence units.

29617824

お薦めの試験操作(参考用のみ)

キナーゼ試験:

[2]

- 合併

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.
細胞試験:

[2]

- 合併
  • 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].


    (参考用のみ)

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。

化学情報

分子量 419.38
化学式

C20H19F2N3O5

CAS No. 1051375-16-6
Storage powder
in solvent
別名 S/GSK1349572
Smiles CC1CCOC2N1C(=O)C3=C(C(=O)C(=CN3C2)C(=O)NCC4=C(C=C(C=C4)F)F)O

投与溶媒組成計算器(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)
投与量 mg/kg 動物平均体重 g 投与体積(動物毎) ul 動物数
ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)
% DMSO % % Tween 80 % ddH2O
計算リセット

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (mg) = 濃度 (mM) x 体積 (mL) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

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

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 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):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

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

モル濃度計算器

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04771754 Not yet recruiting Drug: Dolutegravir HIV-1-infection Chelsea and Westminster NHS Foundation Trust October 1 2021 Phase 1
NCT04166474 Not yet recruiting Drug: Dolutegravir Hiv|Tuberculosis Helen Reynolds|Infectious Disease Institute Kampala Uganda|Desmond Tutu HIV Centre|University of Liverpool October 2021 Phase 4
NCT05006170 Not yet recruiting Drug: DTG DT 20 mg|Drug: DTG DT 25 mg Pediatric HIV Infection Chulalongkorn University August 3 2021 --

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

Integraseシグナル伝達経路

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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