Rilpivirine

利匹韦林,利吡韦林,R-278474,R278474,TMC278,R 278474,TMC 278,TMC-278,

Rilpivirine (利匹韦林; R278474, TMC 278) 是HIV的非核苷逆转录酶抑制剂。

目录号
EY1571
EY1571
EY1571
纯度
99.69%
99.69%
99.69%
规格
5 mg
10 mg
50 mg
原价
610
990
2960
售价
610
990
2960
库存
现货
现货
现货
订购
订购
订购
订购
订购
订购
  • 生物活性

    Rilpivirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI), and used to treat HIV-1 infection.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

  • 动物实验

    4 mg/kg(大鼠);1.25 mg/kg(另一物种)静脉注射,口服

  • 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 AKm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] Janssen PA, et al. J Med Chem. 2005, 48(6), 1901-1909.

    分子式
    C22H18N6
    分子量
    366.42
    CAS号
    500287-72-9
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    70 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
    NCT01562886 HIV Drug: Rilpivirine Imperial College London|Janssen-Cilag Ltd. Phase 1 2012-03-01 2014-05-19
    NCT02494986 Human Immunodeficiency Virus Type 1 Drug: Rilpivirine Janssen Sciences Ireland UC Phase 2 2015-07-01 2016-08-25
    NCT02547870 Human Immunodeficiency Virus Type 1 Drug: Rilpivirine (RPV)|Drug: Rilpivirine Long-Acting Parenteral Formulation (RPVA)|Drug: Aged RPVA Janssen Infectious Diseases BVBA Phase 1 2015-08-01 2016-07-05
    NCT02404233 HIV Positive Drug: darunavir/cobicistat|Drug: rilpivirine Therapeutic Concepts|Janssen Scientific Affairs, LLC Phase 4 2015-03-01 2015-03-30
    NCT01719614 Healthy Participants Drug: Metformin|Drug: Rilpivirine Janssen R&D Ireland Phase 1 2012-10-01 2014-03-05
    NCT02530060 Healthy Drug: Rilpivirine/Tenofovir Disoproxil Fumarate/Emtricitabine FDC Janssen Pharmaceutical K.K. Phase 4 2015-08-01 2016-12-30
    NCT01615614 Healthy Drug: Rilpivirine|Drug: Rifabutin Janssen R&D Ireland Phase 1 2012-04-01 2014-03-27
    NCT03033368 HIV Drug: Rilpivirine Mahidol University|amfAR, The Foundation for AIDS Research Phase 2|Phase 3 2015-07-01 2017-01-24
    NCT01692470 Human Immunodeficiency Virus Type 1 (HIV-1) Infection Drug: No intervention Janssen Pharmaceutica Phase 4 2013-06-01 2015-11-30
    NCT01585038 Cardiovascular Disease Drug: Efavirenz|Drug: Rilpivirine Indiana University|Janssen Services, LLC Phase 4 2012-07-01 2015-07-27
    NCT02165202 Human Immunodeficiency Virus (HIV) Drug: Rilpivirine|Drug: Placebo PATH|Bill and Melinda Gates Foundation|National Institute of Allergy and Infectious Diseases (NIAID)|National Institutes of Health (NIH) Phase 2 2014-10-01 2016-03-14
    NCT01268839 HIV Drug: TMC278|Drug: TMC278|Drug: Efavirenz Tibotec, Inc|Tibotec Therapeutics, a Division of Ortho Biotech Products, L.P., USA Phase 1 2010-01-01 2013-09-02
    NCT02104700 HIV Drug: Rilpivirine/Emtricitabine/Tenofovir Philip Grant|Rwanda Biomedical Center|Gilead Sciences|Stanford University Phase 2|Phase 3 2014-04-01 2015-07-15
    NCT02561936 Healthy Drug: Rilpivirine Oral Tablet|Drug: Rilpivirine formulation G007|Drug: Rilpivirine formulation G009-01|Drug: Rilpivirine formulation G002|Dietary Supplement: Standardized Breakfast Janssen Sciences Ireland UC Phase 1 2015-10-01 2016-06-09
    NCT01049932 HIV Infections Drug: TMC278LA St Stephens Aids Trust Phase 1|Phase 2 2010-03-01 2010-08-13
    NCT01656018 Healthy Drug: TMC278, Long acting (LA) Janssen Research & Development, LLC Phase 1 2012-11-01 2016-04-06
    NCT01266902 HIV-1 Infection Drug: Rilpivirine Janssen R&D Ireland Phase 3 2011-02-25 2017-03-14
    NCT00799864 Human Immuno Deficiency (HIV) Infection Drug: Rilpivirine|Drug: Zidovudine|Drug: Abacavir|Drug: Tenofovir disoproxil fumarate|Drug: Lamivudine|Drug: Emtricitabine Janssen Sciences Ireland UC Phase 2 2011-01-07 2017-03-21
    NCT01975012 HIV Infections Drug: Rilpivirine National Institute of Allergy and Infectious Diseases (NIAID)|National Institute of Mental Health (NIMH) Phase 1|Phase 2 2014-09-01 2015-08-31
    NCT01804244 Healthy Drug: TMC278 Janssen Pharmaceutical K.K. Phase 4 2013-03-01 2014-03-18

    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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