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Ketoconazole

酮康唑

Ketoconazole (酮康唑)是咪唑类抗真菌剂,是经典的CYP3A4抑制剂。

目录号
EY0899
EY0899
EY0899
纯度
99.57%
99.57%
99.57%
规格
100 mg
500 mg
1 g
原价
450
552
945
售价
450
552
945
库存
现货
现货
现货
订购
订购
订购
订购
订购
订购
  • 生物活性

    Ketoconazole inhibits cyclosporine oxidase and testosterone 6 beta-hydroxylase with IC50 of 0.19 mM and 0.22 mM, respectively.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

    25 μM

  • 动物实验

    25 mg/kg 腹腔注射

  • 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] Ayub and Levell (1989) Inhibition of human adrenal steroidogenic enzymes in vitro by imidazole drugs including ketoconazole. J.Steroid Biochem. 32 515.
    [2] Kuhn-Velten et al (1992) Ketoconazole inhibition of the bifunctional cytochrome P450c17 does not affect androgen formation from the endogenous lyase substrate. Biochem.Pharmacol. 44 2371.
    [3] Dumaine et al (1998) Blockade of HERG and Kv1.5 by ketoconazole. J.Pharmacol.Exp.Ther. 286 727.

    分子式
    C26H28Cl2N4O4
    分子量
    531.43
    CAS号
    65277-42-1
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    20 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
    NCT00830388 Tinea Versicolor Drug: Ketoconazole 2% Foam Boni Elewski, MD|University of Alabama at Birmingham Phase 4 2008-11-01 2012-08-21
    NCT01330563 Type 2 Diabetes Mellitus Drug: CKD-501, Ketoconazole Chong Kun Dang Pharmaceutical|Severance Hospital Phase 1 2011-03-01 2011-06-28
    NCT00895310 Prostate Cancer Drug: Ketoconazole University of California, Davis Phase 2 2009-05-01 2016-12-22
    NCT01735240 Asthma,|Pharmacokinetics,|Cmax,|Tmax,|位z,|AUC,|Ketoconazole,|Metabolite Drug: AZD5069|Drug: Ketoconazole AstraZeneca Phase 1 2012-12-01 2015-06-24
    NCT01584297 Granulosa Cell Tumour of the Ovary Drug: Ketoconazole Grupo Espaol de Tumores Hurfanos e Infrecuentes Phase 2 2012-10-01 2015-01-19
    NCT01036594 Prostate Cancer Drug: Ketoconazole, hydrocortisone|Drug: Ketoconazole, dexamethasone University of California, San Francisco Phase 2 2009-12-01 2016-05-22
    NCT01910480 Effect of Ketoconazole on the PK of NBI-98854 in Healthy Subjects Drug: NBI-98854 50 mg capsule once daily|Drug: Ketoconazole 400 mg (200 mg twice daily) Neurocrine Biosciences Phase 1 2013-07-01 2013-09-03
    NCT01154764 Healthy Drug: CG100649|Drug: CG100649 and ketoconazole CrystalGenomics, Inc. Phase 1 2009-10-01 2013-02-13
    NCT00212095 Metastatic Breast Cancer Drug: docetaxel and ketoconazole National University Hospital, Singapore Phase 2 2005-06-01 2012-10-31
    NCT00824863 Pityrosporum Folliculitis Drug: ketoconazole 2% foam Wayne Fujita, M.D.|Fujita, Wayne, M.D. Phase 4 2008-12-01 2014-08-19
    NCT01318265 Pharmacokinetics Drug: Regorafenib (BAY73-4506); Regorafenib (BAY73-4506) plus ketoconazole Bayer Phase 1 2011-03-01 2014-10-31
    NCT01657838 Pharmacokinetics of Isavuconazole|Pharmacokinetics of Ketoconazole|Healthy Adult Volunteers Drug: Isavuconazole|Drug: Ketoconazole Astellas Pharma Global Development, Inc.|Basilea Pharmaceutica International Ltd|Astellas Pharma Inc Phase 1 2012-05-01 2015-08-31
    NCT00388557 Cancer Drug: vinflunine + ketaconazole Bristol-Myers Squibb Phase 1 2005-10-01 2016-09-16
    NCT00404378 Nausea and Vomiting, Chemotherapy-Induced Drug: ketoconazole|Drug: casopitant GlaxoSmithKline Phase 1 2006-10-01 2016-10-26
    NCT00703846 Dermatitis, Seborrheic Drug: Ketoconazole Stiefel, a GSK Company|GlaxoSmithKline Phase 4 2008-06-01 2016-12-01
    NCT01468558 Healthy Drug: MAP0004|Drug: IV DHE|Drug: Ketoconazole Allergan|MAP Pharmaceuticals, Inc., a wholly owned subsidiary of Allergan Phase 1 2010-07-01 2013-12-09
    NCT01896323 Healthy Volunteers Drug: CC-223|Drug: Ketoconazole Celgene Corporation|Celgene Phase 1 2013-07-01 2014-04-03
    NCT01021358 Lymphoma|Chronic Lymphocytic Leukemia|Solid Tumors Drug: ABT-263|Drug: Ketoconazole Abbott Phase 1 2010-01-01 2010-12-16
    NCT00384917 Healthy Drug: Ketoconazole Wyeth is now a wholly owned subsidiary of Pfizer Phase 1 2006-08-01 2009-07-08
    NCT00501397 Type 2 Diabetes Mellitus|Diabetes Mellitus, Type 2 Drug: ketoconazole|Drug: GSK189075 GlaxoSmithKline Phase 1 2007-02-01 2012-05-31

    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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