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Maraviroc

马拉维若,马拉韦若,马拉维诺,UK-427857

Maraviroc是一种趋化因子受体CCR5抑制剂，作用于MIP-1α， MIP-1β和RANTES 时，IC50分别为3.3 nM， 7.2 nM和5.2 nM。

目录号
EY1740
EY1740
EY1740
EY1740
纯度
99.36%
99.36%
99.36%
99.36%
规格
5 mg
10 mg
50 mg
100 mg
原价
520
970
2980
5680
售价
520
970
2980
5680
库存
现货
现货
现货
现货
订购
订购
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  • 生物活性

    Maraviroc (UK-427857) is a selective CCR5 antagonist with potent anti-human immunodeficiency virus type 1 (HIV-1) activity and favorable pharmacological properties.

  • 体外研究

  • 体内研究

    2% DMSO+castor oil

  • 激酶实验

  • 细胞实验

    0-1 μM

  • 动物实验

    ~64 μg25μL凝胶配方小心地加到小鼠的阴道穹窿中。

  • 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] Dorr P, et al. Antimicrob Agents Chemother. 2005, 49(11), 4721-4732.
    [2] Walker, D.K., et al.: Drug Metab. Dispos., 33, 587 (2005)
    [3] Wood, A., et al.: Prog. Med. Chem., 43, 239 (2005).
    [4] Kuritzkes et al (2008) Fresh from the pipeline - maraviroc. Nat.Rev.Drug Discov. 7 15.
    [5] Garcia-Perez et al (2011) New insights into the mechanisms whereby low molecular weight CCR5 ligands inhibit HIV-1 infection. J.Biol.Chem. 286 4978.
    [6] Piotrowska et al (2016) Maraviroc reduces neuropathic pain through polarization of microglia and astroglia - Evidence from in vivo and in vitro studies. Neuropharmacology S0028-3908 30164.

    分子式
    C29H41F2N5O    		 分子量
    513.67    		 CAS号
    376348-65-1    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    100 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    100 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
    NCT02881762 Hepatitis C|Human Immunodeficiency Virus Drug: Maraviroc University of Maryland|ViiV Healthcare Phase 4 2016-09-01 2016-08-26
    NCT00775294 HIV/AIDS Drug: Maraviroc University of North Carolina, Chapel Hill|Pfizer Phase 1 2008-05-01 2011-05-11
    NCT01428986 HIV Infections|AIDS Drug: Maraviroc National Center for Global Health and Medicine, Japan 2009-11-01 2014-09-24
    NCT00948753 Graft-versus-host Disease|Hematopoietic Stem Cell Transplantation Drug: Maraviroc Abramson Cancer Center of the University of Pennsylvania Phase 1|Phase 2 2009-06-01 2016-09-23
    NCT01133210 Hypertriglyceridemia Drug: Maraviroc|Other: placebo Washington University School of Medicine|Pfizer Phase 1 2011-01-01 2013-12-09
    NCT01980329 Cytochrome P450 CYP3A5 Enzyme Polymorphism|Healthy Subjects|Pharmacokinetics of Maraviroc Drug: Maraviroc Johns Hopkins University Phase 1 2013-01-01 2015-04-02
    NCT00944541 HIV Infection|HIV Infections Drug: maraviroc French National Agency for Research on AIDS and Viral Hepatitis|Pfizer Phase 2 2009-09-01 2011-12-21
    NCT01389063 Endothelial Dysfunction Drug: Maraviroc S.F.L. van Lelyveld|UMC Utrecht Phase 4 2012-01-01 2013-12-17
    NCT02934022 HIV Infection Drug: Maraviroc Southern California Institute for Research and Education|Pfizer 2012-06-01 2016-10-13
    NCT02167451 Diagnoses That Require Stem Cell Transplant|Graft Versus Host Disease (GVHD) Drug: Maraviroc Children's Hospital Medical Center, Cincinnati Phase 1|Phase 2 2014-07-01 2016-12-01
    NCT00821535 Human Immunodeficiency Virus (HIV) Infection Drug: maraviroc (Selzentry, Celsentri) ViiV Healthcare|Pfizer Phase 1 2009-02-01 2010-11-15
    NCT02159027 AIDS Dementia Complex Drug: Maraviroc|Drug: Placebo University of Hawaii|ViiV Healthcare|University of Puerto Rico Phase 2|Phase 3 2015-05-01 2017-01-03
    NCT00791700 Human Immunodeficiency Virus (HIV) Drug: Maraviroc ViiV Healthcare|Pfizer Phase 2 2009-04-01 2016-12-21
    NCT01449006 Human Immunodeficiency Virus (HIV)|HIV Associated Neurocognitive Disorders (HAND) Drug: Maraviroc Bruce Brew|ViiV Healthcare|St Vincent's Hospital, Sydney Phase 4 2011-10-01 2016-04-13
    NCT01056874 Healthy|HIV Infections Drug: Digoxin|Drug: Digoxin|Drug: Maraviroc ViiV Healthcare|Pfizer Phase 1 2010-03-01 2011-04-06
    NCT01190293 HIV Infection Drug: Maraviroc St Stephens Aids Trust Phase 4 2010-01-01 2012-04-11
    NCT00709111 HIV Infections Drug: Maraviroc AIDS Clinical Trials Group|National Institute of Allergy and Infectious Diseases (NIAID) 2009-01-01 2016-01-04
    NCT01420523 Human Immunodeficiency Virus|Lipohypertrophy Drug: Raltegravir-Maraviroc French National Institute for Health and Medical Research-French National Agency for Research on AIDS and Viral Hepatitis (Inserm-ANRS)|Merck Sharp & Dohme Corp.|ViiV Healthcare Phase 2 2011-12-01 2015-07-23
    NCT00982878 HIV Infections Drug: Maraviroc Imperial College London|Pfizer Phase 1 2009-09-01 2015-03-23
    NCT00665561 Human Immunodeficiency Virus Drug: Maraviroc along with an optimized background antiretroviral drug regimen|Drug: Optimized background antiretroviral drug regimen without maraviroc ViiV Healthcare|Pfizer 2008-03-01 2017-02-23
    NCT00719823 Human Immunodeficiency Virus Type 1 Drug: Maraviroc ViiV Healthcare|Pfizer Phase 3 2008-08-01 2016-05-03

    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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