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Lopinavir

洛匹那韦,罗平拉韦,洛吡那韦,ABT 378,ABT378,ABT-378

Lopinavir是一种有效的HIV protease(HIV蛋白酶)抑制剂, Ki为1.3 pM。

目录号
EY0808
EY0808
EY0808
纯度
99.35%
99.35%
99.35%
规格
50 mg
100 mg
250 mg
原价
470
775
1400
售价
470
775
1400
库存
现货
现货
现货
订购
订购
订购
订购
订购
订购
  • 生物活性

    Lopinavir is a potent HIV protease inhibitor with Ki of 1.3 pM in a cell-free assay.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

  • 动物实验

    10 mg/kg 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] Sham HL, et al. Antimicrob Agents Chemother, 1998, 42(12), 3218-3224.
    [2] Weemhoff, J.L., et al., Apparent mechanism-based inhibition of human CYP3A in-vitro by lopinavir. J Pharm Pharmacol, 2003. 55(3): p. 381-6.
    [3] Vishnuvardhan, D., et al., Lopinavir: acute exposure inhibits P-glycoprotein; extended exposure induces P-glycoprotein. AIDS, 2003. 17(7): p. 1092-4.

    分子式
    C37H48N4O5
    分子量
    628.8
    CAS号
    192725-17-0
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    125 mg/mL
    Water
    <1 mg/mL
    Ethanol
    125 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
    NCT00771498 HIV Infection|Tuberculosis Drug: Lopinavir Oswaldo Cruz Foundation|Abbott Phase 4 2008-11-01 2015-05-15
    NCT01074931 HIV-1 Infections Drug: Lopinavir/ritonavir (Kaletra) Abbott 2008-04-01 2011-07-07
    NCT01700790 AIDS|Tuberculosis Drug: Lopinavir/ritonavir and ritonavir University of Miami|Oswaldo Cruz Foundation Phase 4 2016-01-01 2016-12-06
    NCT01172535 HIV Drug: Lopinavir/ritonavir National Institute of Allergy and Infectious Diseases (NIAID) Phase 2|Phase 3 2010-11-01 2015-11-16
    NCT01581853 HIV Drug: Lopinavir/ritonavir 800 mg / 200mg Daniel Podzamczer|Hospital Universitari de Bellvitge Phase 4 2012-05-01 2016-10-05
    NCT01002898 HIV Drug: lopinavir/ritonavir soft gel capsule Bamrasnaradura Infectious Diseases Institute Phase 3 2007-04-01 2011-11-10
    NCT00605098 HIV Infections|Pregnancy Drug: Lopinavir / ritonavir|Drug: Lopinavir/ritonavir Oswaldo Cruz Foundation|Ministry of Health, Brazil Phase 4 2008-02-01 2013-10-25
    NCT00621166 HIV Infections Drug: generic lopinavir/ritonavir The HIV Netherlands Australia Thailand Research Collaboration Phase 2 2008-06-01 2012-04-03
    NCT00752037 HIV Infections Drug: lopinavir/ritonavir and raltegravir Saint Michael's Medical Center|Abbott Phase 4 2008-09-01 2011-07-19
    NCT01660477 Pharmacokinetics of Isavuconazole|Pharmacokinetics of Lopinavir/Ritonavir|Healthy Volunteers Drug: Isavuconazole|Drug: Lopinavir/ritonavir Astellas Pharma Global Development, Inc.|Basilea Pharmaceutica International Ltd|Astellas Pharma Inc Phase 1 2012-06-01 2015-02-20
    NCT01139905 HIV-1 Infections Other: lopinavir/ritonavir The HIV Netherlands Australia Thailand Research Collaboration|Chulalongkorn University|UMC St. Radboud, Nijmegen, The Netherlands Phase 2 2010-04-01 2015-03-24
    NCT00619944 HIV Infections Drug: Lumefantrine - lopinavir/ritonavir drug interaction|Drug: Lumefantrine only arm Makerere University|University of Liverpool Phase 4 2008-02-01 2010-12-03
    NCT01237444 HIV Infection Drug: lopinavir/ritonavir plus one nucleoside|Drug: lopinavir /ritonavir plus two nucleosides Pedro Cahn|Abbott|The Huesped Foundation Phase 3 2010-12-01 2012-06-08
    NCT01076972 Human Immunodeficiency Virus Drug: Lopinavir/ritonavir (Kaletra) Abbott 2000-12-01 2012-01-31
    NCT00985543 Acquired Immunodeficiency Syndrome Drug: lopinavir/ritonavir Kirby Institute Phase 1 2009-10-01 2011-03-02
    NCT01076985 Human Immunodeficiency Virus Drug: Lopinavir/ritonavir (Kaletra) Abbott 2000-12-01 2011-12-09
    NCT00344487 HIV Drug: Lopinavir/Ritonavir University of Maryland 2005-12-01 2014-12-17
    NCT00762320 HIV Infections Drug: Low dose Kaletra tablets Phoenix Children's Hospital|Abbott 2008-10-01 2014-02-05
    NCT02348177 Acquired Immunodeficiency Syndrome|Tuberculosis Drug: lopinavir with ritonavir in 1:1 ratio|Drug: Lopinavir/ritonavir 4:1 Drugs for Neglected Diseases|University of Cape Town|Medecins Sans Frontieres, Netherlands|French Development Agency|UBS Optimus Foundation Phase 4 2013-01-01 2015-01-22
    NCT00981318 HIV Infections|Acquired Immunodeficiency Syndrome Drug: lopinavir/ritonavir plus maraviroc Rodwick, Barry M., M.D.|Abbott Phase 4 2009-12-01 2015-06-20
    NCT00159224 HIV Infections Drug: Lopinavir/ritonavir simplification strategy The Huesped Foundation|Abbott Phase 4 2005-04-01 2015-09-04
    NCT00866021 HIV/HCV Co-infection|HIV Infections Drug: Lopinavir/ritonavir|Drug: Lopinavir/ritonavir with two nucleoside analogs Fundacion SEIMC-GESIDA|Abbott Phase 4 2008-02-01 2013-03-21
    NCT01088516 HIV Drug: Lopinavir/Ritonavir (200/50 mg) Tablets + Zidovudine + 3TC University of Zambia|University of Toronto|Abbott Phase 4 2008-12-01 2015-06-22

    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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