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Dolutegravir

度鲁特韦,GSK1349572,GSK 1349572,GSK-1349572

Dolutegravir 是整合酶抑制剂，IC50为2.7 nM，对raltegravir-抗性的突变型Y143R，Q148K，N155H和G140S/Q148H有一定抑制性。

目录号
EY1145
EY1145
EY1145
EY1145
纯度
99.42%
99.42%
99.42%
99.42%
规格
2 mg
5 mg
10 mg
50 mg
原价
720
995
1420
6100
售价
720
995
1420
6100
库存
现货
现货
现货
现货
订购
订购
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  • 生物活性

    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.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

    0-10 μM

  • 动物实验

  • 不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数


    例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

  • 参考文献

    [1] Robert A Smith,et al. In vitro activity of dolutegravir against wild-type and integrase inhibitor-resistant HIV-2. Retrovirology. 2015; 12: 10. Published online 2015 Feb 5. doi: 10.1186/s12977-015-0146-8.
    [2] Thibault Mesplède,et al. Addition of E138K to R263K in HIV integrase increases resistance to dolutegravir, but fails to restore activity of the HIV integrase enzyme and viral replication capacity. J Antimicrob Chemother. 2014 Oct; 69(10): 2733–2740. Published online 2014 Jun 10. doi: 10.1093/jac/dku199.
    [3] Takahiro Seki,et al. Effects of Raltegravir or Elvitegravir Resistance Signature Mutations on the Barrier to Dolutegravir Resistance In Vitro. Antimicrob Agents Chemother. 2015 May; 59(5): 2596–2606. Prepublished online 2015 Feb 17. Published online 2015 Apr 10. doi: 10.1128/AAC.04844-14.

    分子式
    C20H19F2N3O5    		 分子量
    419.38    		 CAS号
    1051375-16-6    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    ≥80 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    <1 mg/mL

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT02487706 HIV Drug: Dolutegravir Fundacio Lluita Contra la SIDA Phase 4 2015-06-01 2015-09-30
    NCT02401828 Human Immunodeficiency Virus Drug: Dolutegravir Erasmus Medical Center Phase 4 2015-03-01 2017-02-06
    NCT01568892 Infection, Human Immunodeficiency Virus Drug: dolutegravir 50 mg twice daily|Drug: dolutegravir placebo twice daily|Drug: Open-label dolutegravir 50mg twice daily ViiV Healthcare|Shionogi|GlaxoSmithKline Phase 3 2012-04-01 2014-01-02
    NCT02491242 HIV Infection Other: Dolutegravir in a dual therapy regimen Asociacion para el Estudio de las Enfermedades Infecciosas 2015-11-01 2017-01-26
    NCT02098837 HIV Drug: Dolutegravir St Stephens Aids Trust Phase 4 2014-04-01 2016-07-26
    NCT03016533 Infection, Human Immunodeficiency Virus Drug: Dolutegravir film-coated tablets|Drug: Dolutegravir film-coated dispersible tablets ViiV Healthcare|PPD Phase 3 2017-08-01 2017-02-28
    NCT02572947 Human Immunodeficiency Virus|Dolutegravir|Monotherapy|Treatment Efficacy Drug: Dolutegravir Calmy Alexandra|University Hospital, Geneva Phase 2 2016-06-01 2016-12-23
    NCT02500446 HIV Drug: dolutegravir|Other: Placebo University of Melbourne|The Alfred|ViiV Healthcare Phase 4 2015-08-01 2016-08-14
    NCT02924389 HIV Drug: dolutegravir|Drug: Triumeq|Drug: Truvada Emory University|National Institutes of Health (NIH) 2016-09-01 2016-10-04
    NCT02211482 HIV-1 Infection Drug: dolutegravir, lamivudine The Huesped Foundation|ViiV Healthcare Phase 4 2014-10-01 2016-08-21
    NCT01328041 Infection, Human Immunodeficiency Virus Drug: dolutegravir ViiV Healthcare|Shionogi|GlaxoSmithKline Phase 3 2011-05-01 2015-12-07
    NCT01353716 Infection, Human Immunodeficiency Virus Drug: Dolutegravir 50 mg ViiV Healthcare|Shionogi|GlaxoSmithKline Phase 1 2011-06-01 2012-04-26
    NCT02551523 Monotherapy|Dolutegravir|Primary HIV Infection|Treatment Efficacy Drug: Dolutegravir|Drug: Standard of care combinational antiretroviral therapy University of Zurich Phase 2 2015-11-01 2016-05-30
    NCT02285374 HIV Drug: Dolutegravir, efavirenz, efavirenz/emtricitabine/tenofovir St Stephens Aids Trust|ViiV Healthcare Phase 4 2014-11-01 2014-11-06
    NCT01498861 Infection, Human Immunodeficiency Virus Drug: Ortho-Cyclen|Drug: Dolutegravir|Drug: Placebo ViiV Healthcare|Shionogi|GlaxoSmithKline Phase 1 2011-12-01 2012-05-17
    NCT02245022 HIV|Pregnancy Drug: Dolutegravir 50mg od|Drug: Standard of Care University of Liverpool|ViiV Healthcare|Makerere University Phase 2|Phase 3 2017-03-14 2017-03-14
    NCT02976259 HIV Infection Primary Drug: Dolutegravir Institut de Mdecine et d'Epidmiologie Applique - Fondation Internationale Lon M'Ba Phase 3 2016-12-01 2016-11-24
    NCT02509195 HIV Drug: Triumeq St Stephens Aids Trust|ViiV Healthcare Phase 4 2015-07-01 2017-03-16

    注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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