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Tolcapone

托卡朋,Ro 40-7592

Tolcapone是一种有效和选择性的可逆硝基酚类儿茶酚-O-甲基转移酶(COMT)抑制剂,Ki为30nM。

目录号
EY1061
EY1061
EY1061
EY1061
EY1061
纯度
99.31%
99.31%
99.31%
99.31%
99.31%
规格
1 mg
5 mg
10 mg
50 mg
100 mg
原价
150
290
492
1100
1550
售价
150
290
492
1100
1550
库存
现货
现货
现货
现货
现货
订购
订购
订购
订购
订购
订购
  • 生物活性

    Tolcapone is a selective, potent and reversible of catechol-O-methyl transferase (COMT) inhibitor with Ki of 30 nM.

  • 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 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] Ricardo Sant'Anna,et al. Repositioning tolcapone as a potent inhibitor of transthyretin amyloidogenesis and associated cellular toxicity. Nat Commun. 2016; 7: 10787. Published online 2016 Feb 23. doi: 10.1038/ncomms10787.
    [2] Aqilah M. McCane,et al. Tolcapone suppresses ethanol intake in alcohol preferring rats performing a novel cued access protocol. Alcohol Clin Exp Res. Author manuscript; available in PMC 2015 Sep 1. Published in final edited form as: Alcohol Clin Exp Res. 2014 Sep; 38(9): 2468–2478. doi: 10.1111/acer.12515.
    [3] Sophia C. Magalona,et al. Inhibition of Comt with tolcapone slows progression of polycystic kidney disease in the more severely affected PKD/Mhm (cy/+) substrain of the Hannover Sprague-Dawley rat. CNS Drugs. Author manuscript; available in PMC 2014 Aug 18.

    分子式
    C14H11NO5
    分子量
    273.24
    CAS号
    134308-13-7
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    55 mg/mL
    Water
    <1 mg/mL
    Ethanol
    55 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
    NCT00927563 Pathological Gambling Drug: Tolcapone University of Chicago Phase 2 2009-06-01 2014-01-17
    NCT02630043 Neuroblastoma Drug: Tolcapone|Drug: Oxaliplatin Spectrum Health Hospitals Phase 1 2015-12-01 2016-09-14
    NCT02740582 Alcohol Abuse|Impulsive Behavior Drug: Tolcapone|Drug: Placebo University of California, San Francisco 2016-10-01 2017-01-12
    NCT01202955 Nicotine Dependence Drug: Tolcapone|Drug: Placebo University of Pennsylvania Phase 2 2008-07-01 2011-05-04
    NCT02652598 Brain Injuries, Traumatic|Neurocognitive Disorders|Brain Injuries Drug: Tolcapone Sheppard Pratt Health System|Lieber Institute for Brain Development (LIBD) Phase 2 2015-11-01 2017-01-17
    NCT02080715 Healthy Drug: Tolcapone|Drug: Placebo University of Zurich Phase 1 2013-06-01 2014-09-11
    NCT00604591 Frontotemporal Lobar Degeneration Drug: Tolcapone|Drug: Placebo Columbia University|National Institute of Neurological Disorders and Stroke (NINDS) Phase 2 2011-07-01 2016-06-14
    NCT00044083 Schizophrenia Drug: Tolcapone National Institute of Mental Health (NIMH)|National Institutes of Health Clinical Center (CC) Phase 2 2002-08-01 2016-08-31
    NCT00033059 Cocaine-Related Disorders Drug: Tolcapone National Institute on Drug Abuse (NIDA) Phase 1 2001-07-01 2017-01-10
    NCT02448654 Nicotine Dependence Drug: Tolcapone|Drug: Sugar Pill Yale University|VA Office of Research and Development 2015-10-01 2016-07-18
    NCT02191826 Familial Amyloid Polyneuropathy (FAP) Drug: SOM0226 SOM Biotech SL|Hospital Vall d'Hebron Phase 1|Phase 2 2014-07-01 2016-11-29
    NCT02949934 Alcohol Use Disorder Drug: Tolcapone|Drug: Placebo Medical University of South Carolina|National Institute on Alcohol Abuse and Alcoholism (NIAAA) Phase 2 2016-05-01 2016-10-27
    NCT01001520 Tobacco Use Disorder Drug: Tolcapone|Drug: Placebo University of Pennsylvania|National Institute on Drug Abuse (NIDA) Phase 2 2010-01-01 2014-05-29
    NCT02929485 Addiction Drug: Tolcapone|Drug: Placebo|Drug: Bromocriptine University of California, San Francisco|University of California, Berkeley 2013-07-01 2016-10-10
    NCT02772978 Pathological Gambling Drug: Tolcapone|Drug: Placebo University of California, San Francisco|National Center for Responsible Gaming 2014-08-01 2016-05-12
    NCT02260570 Mild Traumatic Brain Injury Drug: Tolcapone|Drug: Placebo VA Office of Research and Development|University of California, Berkeley|University of California, San Francisco 2015-08-01 2017-03-13
    NCT01158950 Impulsive Behavior Drug: Tolcapone|Other: Placebo|Drug: Entacapone University of California, San Francisco|University of California, Berkeley|United States Department of Defense 2010-03-01 2016-04-12
    NCT00906828 Parkinson Disease Drug: levodopa/carbidopa|Drug: entacapone|Drug: tolcapone Uppsala University|Swedish Parkinson's Disease Foundation|Swedish Society for Medical Research Phase 4 2008-10-01 2010-01-15
    NCT02994719 Parkinson's Disease|Parkinsonian Disorders|Atypical Parkinson Disease|Progressive Supranuclear Palsy|Multiple System Atrophy|Corticobasal Degeneration|Gait, Frontal Drug: Anti-Parkinson medication|Device: Deep Brain Stimulation Beth Israel Deaconess Medical Center 2016-03-01 2017-03-09

    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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