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Aprepitant

阿瑞匹坦,阿瑞吡坦,阿瑞比坦,MK0869,MK 0869,MK-0869,L-754030,L754030,L 754030

Aprepitant属于SPA类化合物,能阻断神经激肽1(NK1)受体。

目录号
EY1697
EY1697
EY1697
EY1697
EY1697
纯度
99.33%
99.33%
99.33%
99.33%
99.33%
规格
1 mg
5 mg
10 mg
50 mg
100 mg
原价
290
645
896
3210
4420
售价
290
645
896
3210
4420
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

    Aprepitant is a potent and selective neurokinin-1 receptor antagonist.

  • 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] Tattersall FD, et al. Neuropharmacology, 2000, 39(4), 652-663.

    分子式
    C23H21F7N4O3
    分子量
    534.43
    CAS号
    170729-80-3
    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
    15 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
    NCT01963793 Pruritus Drug: Aprepitant|Drug: Placebo LEO Pharma Phase 2 2013-10-01 2014-10-06
    NCT02154360 HIV Infection Drug: Aprepitant University of Pennsylvania Phase 1 2014-05-01 2016-06-01
    NCT01402024 Chemotherapy Induced Nausea and Vomiting Drug: Aprepitant|Drug: Placebo All India Institute of Medical Sciences, New Delhi|Dr. Reddy's Laboratories Limited Phase 3 2011-08-01 2015-01-16
    NCT01074255 Chemotherapy-induced Nausea and Vomiting Drug: EMEND Merck Sharp & Dohme Corp. 2007-04-01 2015-04-02
    NCT01661335 Nausea|Vomiting|Childhood Cancer Drug: Ondansetron, dexamethasone, aprepitant|Drug: Ondansetron, Dexamethasone, placebo University of Oklahoma Phase 3 2012-06-01 2014-12-02
    NCT02161991 Carcinoma, Non-small Cell Lung Drug: Aprepitant|Drug: placebo Hunan Province Tumor Hospital Phase 3 2014-06-01 2016-02-14
    NCT01527994 Opioid Dependence Drug: Aprepitant|Drug: Placebo pill New York University|National Institute on Drug Abuse (NIDA) Phase 1 2012-01-01 2015-04-13
    NCT01012336 Chemotherapy-Induced Nausea and Vomiting|Ovarian Cancer Drug: Aprepitant/Ramosetron/Dexamethasone Samsung Medical Center|Merck Sharp & Dohme Corp. Phase 2 2010-05-01 2012-10-08
    NCT01149369 Gastroparesis Drug: Aprepitant|Drug: Placebo National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK) Phase 3 2013-04-01 2016-03-18
    NCT01249001 Nausea|Vomiting|Chemotherapy Drug: Oral Aprepitant|Drug: Aprepitant The Hospital for Sick Children Phase 2 2010-10-01 2017-02-22
    NCT01683552 ITCH Drug: Aprepitant|Drug: Prednisone|Drug: Fexofenadine Campus Bio-Medico University Phase 2 2010-09-01 2012-09-11
    NCT01334086 Acute Myeloid Leukemia Drug: Aprepitant University Health Network, Toronto|Merck Sharp & Dohme Corp. Phase 2 2011-09-01 2015-06-19
    NCT02532634 Cancer|Tumors Drug: ramosetron, aprepitant, dexamethasone|Drug: palonosetron, aprepitant, dexamethasone Kangdong Sacred Heart Hospital|The Catholic University of Korea|Astellas Pharma Korea, Inc. Phase 4 2015-08-01 2016-08-30
    NCT00999544 Narcotic Abuse Drug: Aprepitant|Drug: Placebo|Drug: Oxycodone University of Kentucky|National Institute on Drug Abuse (NIDA)|Merck Sharp & Dohme Corp. 2009-10-01 2013-07-19
    NCT00819039 Postoperative Nausea and Vomiting Drug: Aprepitant|Drug: Ondansetron Merck Sharp & Dohme Corp. Phase 1 2009-01-01 2015-06-08
    NCT01897337 Postoperative Nausea and Vomiting Drug: Aprepitant|Drug: placebo Yonsei University Phase 4 2012-06-01 2013-07-08
    NCT00717054 Nausea|Vomiting Drug: Aprepitant|Drug: Scopolamine Drexel University|Merck Sharp & Dohme Corp. 2008-02-01 2014-05-01
    NCT02097823 Chemotherapy Induced Nausea and Vomiting Drug: Olanzapine|Drug: Aprepitant Indiana University Phase 2 2014-02-01 2014-03-24
    NCT02347878 Leukemia|Lymphoma Drug: Aprepitant Sun Yat-sen University Phase 4 2015-04-01 2015-01-26
    NCT00970905 Nausea|Vomiting Drug: aprepitant|Drug: Ondansetron University of Vermont|Mayo Clinic|Wake Forest University Health Sciences|Norris Cotton Cancer Center|University of Massachusetts, Worcester Phase 2 2009-10-01 2015-12-27
    NCT02646020 Non-small Cell Lung Cancer Drug: Aprepitant and placebo|Drug: desloratadine and placebo Sun Yat-sen University Phase 2 2015-12-01 2016-01-02
    NCT02939287 Nausea|Vomiting Drug: Aprepitant|Drug: Olanzapine Rush University Medical Center Phase 3 2016-11-01 2016-10-18
    NCT00314743 Nausea|Vomiting Drug: Ondansetron|Drug: Dexamethasone|Drug: Aprepitant Washington University School of Medicine Early Phase 1 2005-10-01 2013-05-22
    NCT01874119 Chemotherapy-induced Nausea and Vomiting Drug: Fosaprepitant St. Louis University|Merck Sharp & Dohme Corp. Phase 2 2013-09-01 2016-10-12
    NCT00888329 Postoperative Nausea and Vomiting Drug: Aprepitant|Drug: Placebo Mayo Clinic Phase 4 2007-07-01 2012-03-05

    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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