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Probenecid

丙磺舒,羧苯磺丙胺,Benemid

Probenecid是一种经典的有机阴离子运输竞争性抑制剂,同时也是一种瞬时感受器电位香草素受体亚家族2(TRPV2)的激动剂和人苦味觉感受器TAS2R16的抑制剂。

目录号
EY0888
EY0888
EY0888
纯度
99.44%
99.44%
99.44%
规格
500 mg
1 g
5 g
原价
320
432
620
售价
320
432
620
库存
现货
现货
现货
订购
订购
订购
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  • 生物活性

    Probenecid is a classical competitive inhibitor of organic anion transport, which is also a TRPV2 agonist and an inhibitor of TAS2R16.

  • 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] McDonough PM, et al. Cell Calcium, 1989, 10(3), 171-180.
    [2] Hammond et al (2007) Glutathione export during apoptosis requires functional multidrug resistance-associated proteins. J.Biol.Chem. 282 14337.
    [3] Silverman et al (2008) Probenecid, a gout remedy, inhibits pannexin 1 channels. Am.J.Physiol.Cell Physiol. 295 C761.
    [4] Ishikawa et al (2010) Function and expression of ATP-binding cassette transporters in cultured human Y79 retinoblastoma cells. Biol.Pharm.Bull. 33 504.

    分子式
    C13H19NO4S
    分子量
    285.36
    CAS号
    57-66-9
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    56 mg/mL
    Water
    <1 mg/mL
    Ethanol
    20 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
    NCT01428284 Healthy Drug: Canagliflozin/Probenecid Johnson & Johnson Pharmaceutical Research & Development, L.L.C. Phase 1 2011-08-01 2012-02-16
    NCT01029782 Cellulitis Drug: IV cefazolin plus oral probenecid and placebo cephalexin|Drug: Oral cephalexin and saline IV plus probenecid placebo Kelowna General Hospital|Canadian Society of Hospital Pharmacists|Capital Health, Canada|Interior Health Authority, Canada Phase 2 2010-05-01 2015-01-13
    NCT01814319 Systolic Heart Failure Drug: Probenecid 1 gr oral twice daily|Drug: Placebo University of Cincinnati Phase 2 2013-03-01 2015-08-24
    NCT00842400 Obesity Drug: Metformin, VI-0521, Sitagliptan, Probenecid VIVUS, Inc. Phase 1 2009-02-01 2010-01-20
    NCT02243631 Calcium Pyrophosphate Deposition Disease Drug: Probenecid VA Office of Research and Development Early Phase 1 2014-10-01 2017-01-04
    NCT01937026 Healthy Volunteers Drug: Baricitinib|Drug: Probenecid Eli Lilly and Company Phase 1 2013-09-01 2013-12-03
    NCT00000670 HIV Infections Drug: Probenecid|Drug: Zidovudine National Institute of Allergy and Infectious Diseases (NIAID) 2012-03-15
    NCT00000706 HIV Infections Drug: Quinine sulfate|Drug: Probenecid|Drug: Zidovudine National Institute of Allergy and Infectious Diseases (NIAID) 2012-03-15
    NCT00024245 Unspecified Adult Solid Tumor, Protocol Specific Drug: pralatrexate|Drug: probenecid Memorial Sloan Kettering Cancer Center|National Cancer Institute (NCI) Phase 1 2001-05-01 2013-06-25
    NCT01907373 Drug Interaction of Olmesartan in Healthy Chinese Volunteers Drug: olmesartan medoxomil|Drug: olmesartan medoxomil+probenecid Central South University Phase 4 2009-08-01 2013-07-24
    NCT00610532 Epilepsy Drug: phenytoin|Drug: phenytoin and probenecid Jim McAuley|Ohio State University Phase 4 2006-03-01 2013-05-13
    NCT01634100 Healthy Drug: Probenecid|Drug: Rifampicin|Drug: Empagliflozin|Drug: Empagliflozin|Drug: Rifampicin|Drug: Probenecid|Drug: Empagliflozin (BI 10773) Boehringer Ingelheim Phase 1 2012-06-01 2014-06-27
    NCT00304434 Influenza Drug: Oseltamivir|Drug: Probenecid VA Office of Research and Development|Brooke Army Medical Center|National Institutes of Health (NIH) Phase 4 2005-02-01 2009-09-21
    NCT00323219 Cellulitis Drug: Cefazolin and Moxifloxacin University of British Columbia Phase 3 2004-01-01 2012-02-06
    NCT00690014 Kidney Disease Drug: probenecid University of Maryland|National Institutes of Health (NIH) 2007-08-01 2008-06-03
    NCT00439530 Avian Influenza A Virus Drug: oseltamivir|Drug: probenecid Mahidol University|National Institute of Allergy and Infectious Diseases (NIAID)|Southeast Asia Influenza Clinical Research Network Phase 1 2006-11-01 2009-07-24
    NCT01322009 Pediatric Traumatic Brain Injury Drug: Probenecid and N-acetyl cysteine|Drug: Placebo University of Pittsburgh|National Institutes of Health (NIH)|National Institute of Neurological Disorders and Stroke (NINDS) Phase 1|Phase 2 2011-03-01 2016-07-01
    NCT01816646 Blood And Marrow Transplantation Drug: Cidofovir|Drug: Probenecid M.D. Anderson Cancer Center|Gilead Sciences Phase 1 2013-09-01 2016-12-02
    NCT01021020 Healthy Drug: Colchicine|Drug: Colchicine|Drug: Colchicine/Probenecid Mutual Pharmaceutical Company, Inc. Phase 1 2007-09-01 2009-12-01
    NCT00002437 Cytomegalovirus Retinitis|HIV Infections Drug: Cidofovir|Drug: Probenecid Gilead Sciences|NIH AIDS Clinical Trials Information Service Phase 2 2005-06-23

    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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