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Etravirine

依曲韦林,R 165335,R165335,R-165335,TMC 125,TMC-125,TMC125,

Etravirine是非核苷类逆转录酶抑制剂，对野生型HIV-1的EC50为1.4 nM到4.8 nM。

目录号
EY1538
EY1538
EY1538
纯度
99.59%
99.59%
99.59%
规格
5 mg
10 mg
50 mg
原价
620
998
2668
售价
620
998
2668
库存
现货
现货
现货
订购
订购
订购
订购
订购
订购
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  • 生物活性

    Etravirine (TMC125) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used for the treatment of HIV.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

  • 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] Das K, et al. J Med Chem, 2004, 47(10), 2550-2560.

    分子式
    C20H15BrN6O    		 分子量
    435.28    		 CAS号
    269055-15-4    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    >5 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
    NCT00959894 HIV Infections Drug: Etravirine (Intelence)|Drug: Truvada University of North Carolina, Chapel Hill|Janssen Pharmaceuticals Phase 2 2009-09-01 2016-04-29
    NCT00855088 HIV/AIDS|HIV Infections Drug: darunavir|Drug: Ritonavir|Drug: Etravirine University of North Carolina, Chapel Hill|Tibotec Pharmaceutical Limited Phase 1 2009-07-01 2011-05-11
    NCT01090648 HIV-Infections Drug: etravirine Tibotec Pharmaceuticals, Ireland Phase 1 2010-03-01 2012-12-10
    NCT02818348 HIV-1 Infection Drug: darunavir/cobicistat|Drug: etravirine Fundacio Lluita Contra la SIDA Phase 1 2016-06-01 2016-12-05
    NCT00855413 Acute HIV Infection|HIV Infections Drug: Darunavir/Ritonavir and Etravirine University of North Carolina, Chapel Hill|Janssen Pharmaceuticals Phase 4 2009-03-01 2014-10-14
    NCT01347658 HIV Dietary Supplement: Echinacea purpurea Fundacio Lluita Contra la SIDA Phase 1 2011-04-01 2011-09-29
    NCT01422330 Human Immunodeficiency Virus (HIV) Infection Drug: Etravirine Janssen R&D Ireland Phase 4 2011-09-01 2014-10-10
    NCT01121809 HIV-1 Infection|HIV Infections Drug: Raltegravir|Drug: Etravirine Hospitales Universitarios Virgen del Roco Phase 4 2010-04-01 2011-02-07
    NCT01625169 HIV Drug: Etravirine pharmacokinetics in breast milk and plasma University of Southern California|Tibotec Therapeutics, a Division of Ortho Biotech Products, L.P., USA 2010-04-01 2014-08-11
    NCT00354627 HIV-1 Drug: TMC125 Tibotec Pharmaceuticals, Ireland Phase 3 2006-01-01 2015-06-11
    NCT00980538 HIV Infections|HIV-1 Drug: Etravirine Janssen R&D Ireland Phase 3 2009-12-01 2017-02-13
    NCT02212379 HIV-1 Infection Drug: raltegravir and etravirine French National Institute for Health and Medical Research-French National Agency for Research on AIDS and Viral Hepatitis (Inserm-ANRS)|Merck Sharp & Dohme Corp.|Janssen-Cilag Ltd. Phase 2 2015-01-01 2016-08-17
    NCT00871234 Endothelial Function|Lipids|Insulin Resistance|Inflammation|HIV Infections Drug: Etravirine Indiana University|Tibotec Therapeutics, a Division of Ortho Biotech Products, L.P., USA Phase 1 2009-04-01 2011-01-05
    NCT01034917 HIV Drug: Etravirine 400 mg dissolved in water every 24 hours|Drug: Continue with the same antiretroviral regimen Germans Trias i Pujol Hospital Phase 3 2009-12-01 2012-10-24
    NCT01427504 Hepatitis C|HIV Drug: boceprevir; etravirine University of Colorado, Denver 2011-08-01 2013-06-04
    NCT00531323 HIV Infections Drug: TMC125 once daily|Drug: TMC125 twice daily St Stephens Aids Trust Phase 1 2007-09-01 2008-09-04
    NCT00903682 HIV Infection|HIV|Acquired Immunodeficiency Syndrome Drug: etravirine (ETR, TMC125)|Drug: efavirenz (EFV) Janssen-Cilag International NV Phase 2 2009-06-01 2013-01-07
    NCT00665847 HIV-1 Drug: Etravirine (TMC125)|Drug: Optimized background regimen (OBR) Tibotec Pharmaceuticals, Ireland Phase 2 2008-11-01 2015-04-02
    NCT00792584 Sleep Disorders Drug: etravirine|Drug: efavirenz University Hospital, Geneva|University of Bern|University of Lausanne Hospitals|Hospital Lugano|University Hospital, Basel, Switzerland|Hospital of Neuchtel 2008-11-01 2011-09-09
    NCT00128830 Human Immunodeficiency Virus Type 1 Drug: Etravirine (ETR)|Drug: Nucleotide reverse transcriptase inhibitors (NRTIs)|Drug: Protease inhibitors (PIs)|Drug: Enfuvirtide (ENF) Tibotec Pharmaceuticals, Ireland Phase 2 2005-06-01 2013-06-10
    NCT00920296 Healthy Subjects|Infection, Human Immunodeficiency Virus Drug: GSK1265744 GlaxoSmithKline Phase 1 2009-07-01 2010-08-30
    NCT00855335 HIV|HIV Infections|Pregnancy Drug: Darunavir|Drug: Ritonavir|Drug: Etravirine|Drug: Rilpivirine|Drug: Darunavir/Cobicistat (FDC) Janssen Scientific Affairs, LLC Phase 3 2009-04-01 2017-02-14
    NCT00081978 HIV Infection Drug: TMC125 Tibotec Pharmaceuticals, Ireland Phase 2 2004-03-01 2010-04-26
    NCT01741844 Acquired Immune Deficiency Syndrome Drug: No intervention Janssen Korea, Ltd., Korea Phase 4 2012-09-01 2016-03-31
    NCT00255099 HIV Drug: TMC125|Drug: Placebo Tibotec Pharmaceuticals, Ireland Phase 3 2005-12-01 2011-06-02

    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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