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Elvitegravir

埃替格韦,埃替拉韦,JTK-303,JTK 303,JTK303,GS-9137,GS 9137,GS9137,

Elvitegravir (EVG, JTK-303/GS-9137)是HIV整合酶抑制剂，对HIV-1 IIIB，HIV-2 EHO和HIV-2 ROD的IC50分别为0.7 nM，2.8 nM和1.4 nM。

目录号
EY1540
EY1540
EY1540
纯度
99.27%
99.27%
99.27%
规格
5 mg
10 mg
50 mg
原价
540
860
3280
售价
540
860
3280
库存
现货
现货
现货
订购
订购
订购
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  • 生物活性

    Elvitegravir (GS-9137, JTK-303) is an HIV integrase inhibitor for HIV-1 IIIB, HIV-2 EHO and HIV-2 ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM in cell-free assays, respectively.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

    0.5 nM-0.1

  • 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] Shimura K, et al. J Virol. 2008, 82(2), 764-774.

    分子式
    C23H23ClFNO5    		 分子量
    447.88    		 CAS号
    697761-98-1    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    ≥85 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    35 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
    NCT02251236 HIV Drug: Stribild|Drug: Genvoya University of California, San Diego|Gilead Sciences|University at Buffalo 2016-01-01 2016-10-24
    NCT00708162 HIV Infection Drug: Elvitegravir|Drug: Raltegravir|Drug: EVG placebo|Drug: RAL placebo|Drug: Background regimen Gilead Sciences Phase 3 2008-07-01 2016-04-21
    NCT01929759 HIV Disease Drug: Stribild (elvitegravir, cobicistat, emtricitabine and tenofovir) Massachusetts General Hospital|Brigham and Women's Hospital|Gilead Sciences 2014-01-01 2015-10-26
    NCT02199613 HIV Infection Drug: Treatment simplification University of British Columbia|Gilead Sciences Phase 4 2014-10-01 2016-06-16
    NCT01923311 Acquired Immune Deficiency Syndrome (AIDS)|HIV Infections Drug: EVG|Drug: Background regimen Gilead Sciences Phase 2|Phase 3 2013-08-01 2016-11-18
    NCT02219217 HIV Drug: Dolutegravir, Elvitegravir and Cobicistat St Stephens Aids Trust|ViiV Healthcare Phase 1 2014-10-01 2016-08-12
    NCT02198443 HIV Drug: Tenofovir + emtricitabine (Truvada),+lopinavir/ritonavir (Kaletra)|Drug: elvitegravir/cobicistat/emtricitabine/Tenofovir-Disoproxil Fundacion Clinic per a la Recerca Biomdica Phase 4 2015-06-06 2017-02-20
    NCT01721109 Acquired Immunodeficiency Syndrome|HIV Infections Drug: EVG/COBI/FTC/TDF Gilead Sciences Phase 2|Phase 3 2012-12-01 2016-12-08
    NCT01533259 Acquired Immunodeficiency Syndrome|HIV Infections Drug: Stribild Gilead Sciences Phase 3 2012-01-01 2015-01-16
    NCT02383108 HIV Infection Drug: EVG +DRV/r|Drug: SOC PENTA Foundation Phase 2|Phase 3 2016-06-01 2016-09-15
    NCT01854775 Acquired Immune Deficiency Syndrome (AIDS)|HIV Infections Drug: E/C/F/TAF Gilead Sciences Phase 2|Phase 3 2013-05-01 2016-12-05
    NCT02882230 HIV Drug: prescription of at least one of the following drugs: rilpivirine, elvitegravir, dolutegravir Fondation Ophtalmologique Adolphe de Rothschild 2016-09-01 2016-08-26
    NCT01495702 Acquired Immunodeficiency Syndrome|HIV Infections Drug: NNRTI|Drug: FTC/TDF|Drug: Stribild Gilead Sciences Phase 3 2011-12-01 2015-12-01
    NCT01967940 HIV|HIV Infections|Acquired Immunodeficiency Syndrome Drug: TAF|Drug: Placebo to match TAF|Drug: E/C/F/TAF|Drug: Pre-existing ARV regimen|Drug: ATV Gilead Sciences Phase 3 2013-10-01 2017-01-12
    NCT02616783 HIV-1 Infection Drug: E/C/F/TAF|Drug: TDF|Drug: FTC|Drug: FTC/TDF|Drug: 3TC|Drug: Third agent Gilead Sciences Phase 3 2015-12-22 2017-02-14
    NCT02180438 HIV-2 Infection Drug: Stribild (Elvitegravir/Cobicistat/Emtricitabine/Tenofovir DF) 1 tablet daily X 48 weeks University of Washington|Clinique des Maladies Infectieuses Ibrahima DIOP Mar/CRCF, Centre Hospitalier Universitaire de Fann|Gilead Sciences Phase 4 2014-09-01 2016-03-04
    NCT02616029 HIV-1 Infection Drug: E/C/F/TAF Gilead Sciences Phase 3 2015-12-17 2017-02-17
    NCT01475838 Acquired Immunodeficiency Syndrome|HIV Infections Drug: PI|Drug: RTV|Drug: FTC/TDF|Drug: Stribild Gilead Sciences Phase 3 2011-11-01 2016-05-06
    NCT00298350 HIV|HIV-1|Human Immunodeficiency Virus Drug: GS-9137 - A Novel HIV-1 Integrase Inhibitor Gilead Sciences Phase 2 2006-02-01 2008-07-28
    NCT01968551 HIV-1|HIV Infections|Acquired Immunodeficiency Syndrome Drug: E/C/F/TAF|Drug: DRV|Drug: Pre-existing ARV regimen Gilead Sciences Phase 3 2013-09-01 2016-09-14
    NCT02351908 HIV Drug: Stribild (Tenofovir Disoproxil Fumarate, Elvitegravir, Cobicistat)|Drug: Isentress (Raltegravir 400 mg)1 tablet twice a day + Truvada (FTC & Tenofovir) 1 tablet|Drug: Tivicay (Dolutegravir 50 mg) 1 tablet once a day + Truvada (FTC & Tenofovir) St Stephens Aids Trust|Merck Sharp & Dohme Corp. Phase 4 2015-03-01 2016-05-24
    NCT00445146 HIV Infections Drug: EVG|Drug: RTV|Drug: ARV regimen Gilead Sciences Phase 2 2007-02-01 2016-03-23
    NCT02220868 Hepatitis C Infection|HIV Infection Drug: Sofosbuvir, Ribavirin, and Stribild Saint Michael's Medical Center Phase 4 2014-07-01 2016-08-03
    NCT01694420 HIV Drug: (FDC) ELV/COBI/FTC/TDF Duke University Phase 3 2012-09-01 2017-01-03
    NCT02477527 HIV|AIDS|Sleep Disorders Drug: elvitegravir/ cobicistat/ emtricitabine/ tenofovir disoproxil Midtown Medical Center, Tampa, FL|Gilead Sciences Phase 4 2015-02-01 2016-03-21

    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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