Lovastatin

洛伐他汀,洛伐司他汀,MK-803

Lovastatin (洛伐他汀) 是高效HMG-CoA还原酶抑制剂,IC50为3.4 nM,有降血脂作用。

目录号
EY0850
EY0850
EY0850
EY0850
纯度
99.15%
99.15%
99.15%
99.15%
规格
5 mg
10 mg
50 mg
100 mg
原价
180
325
580
885
售价
180
325
580
885
库存
现货
现货
现货
现货
订购
订购
订购
订购
订购
订购
  • 生物活性

    Lovastatin is an inhibitor of HMG-CoA reductase with IC50 of 3.4 nM, used for lowering cholesterol (hypolipidemic agent). Decreases CDK2, 4, 6 and cyclin E levels and induces G1 arrest and apoptosis in tumor cell lines in vitro. Inactive lactam prodrug of lovastatin hydroxy acid, naturally bioactivated in vivo.

  • 体外研究

  • 体内研究

    30% PEG400+0.5% Tween80+5% propylene glycol

  • 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] Pahan K, et al. J Clin Invest, 1997, 100(11), 2671-2679.
    [2] Mendola, C.E. and Backer, J.M. 1990. Cell Growth Differ. 1: 499-502.
    [3] Vincent, T.S., et al. 1991. Biochem. Biophys. Res. Commun. 180: 1284-1289.
    [4] Rubins, J.B., et al. 1998. Am. J. Respir. Crit. Care Med. 157: 1616-1622.
    [5] Bobek, P., et al. 1998. Nutrition. 14: 282-286.
    [6] Kim, W.S., et al. 2001. Invest New Drugs. 19: 81-83.

    分子式
    C24H36O5
    分子量
    404.54
    CAS号
    75330-75-5
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    10 mg/mL
    Water
    <1 mg/mL
    Ethanol
    10 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
    NCT00285857 Breast Cancer Drug: Lovastatin Stanford University Phase 2 2005-11-01 2017-01-19
    NCT00580970 Prostate Cancer Drug: lovastatin Virginia Commonwealth University|Hunter Holmes Mcguire Veteran Affairs Medical Center Phase 2 2007-04-01 2016-09-28
    NCT00585052 Ovarian Cancer Drug: Lovastatin and Paclitaxel University of Iowa Phase 2 2003-08-01 2010-12-20
    NCT01527669 Healthy Subjects Drug: LipoCol Forte capsules|Drug: Lovastatin Tablet National Taiwan University Hospital|National Science Council, Taiwan Phase 4 2012-02-01 2012-07-09
    NCT01478828 Prostate Cancer Drug: Lovastatin Sidney Kimmel Comprehensive Cancer Center 2012-03-01 2015-10-13
    NCT01346670 Healthy Volunteer Drug: LipoCol and Mevacor Taipei Medical University WanFang Hospital Phase 4 2006-10-01 2011-05-01
    NCT00963664 Melanoma|Malignant Melanoma Drug: lovastatin|Drug: interferon alfa-2b NeoPlas Innovation Phase 2 2009-12-01 2009-09-04
    NCT00700921 Chronic Obstructive Pulmonary Disease (COPD) Drug: Lovastatin|Drug: Placebo National Jewish Health|National Heart, Lung, and Blood Institute (NHLBI) Phase 2 2008-04-01 2012-11-26
    NCT00302952 Rheumatoid Arthritis Drug: Lovastatin|Drug: Placebo National Institute of Allergy and Infectious Diseases (NIAID)|Autoimmunity Centers of Excellence Phase 2 2006-08-01 2016-09-13
    NCT02642653 Fragile X Syndrome|Genetic Diseases Drug: Lovastatin|Drug: Placebo Randi J. Hagerman, MD|University of California, Davis Phase 4 2016-01-01 2016-10-24
    NCT00352599 Neurofibromatosis 1 Drug: Lovastatin|Drug: Lovastatin|Drug: placebo pill University of California, Los Angeles Phase 1 2009-09-01 2016-11-18
    NCT00584012 Any Cancer|Breast Cancer Drug: Lovastatin and Docetaxel University of Iowa Phase 1|Phase 2 2004-04-01 2009-06-18
    NCT02603770 Lipid Metabolism Disorder Drug: XueZhiKang|Drug: Lovastatin Luye Pharma Group Ltd. Phase 1 2015-11-01 2016-12-02
    NCT00583102 Acute Myeloid Leukemia Drug: Lovastatin and Cytarabine University of Iowa Phase 1|Phase 2 2001-06-01 2010-12-20
    NCT01110642 Syndromic Ichthyoses|CHILD Syndrome|Smith Lemli Opitz Syndrome|Conradi Syndrome Drug: Lovastatin Northwestern University Phase 2 2011-07-01 2015-05-15
    NCT00243880 Stroke Drug: lovastatin Columbia University Phase 1 2005-09-01 2016-05-05
    NCT00689806 Severe Persistent Asthma Drug: Lovastatin|Drug: Placebo University of Chicago Phase 1|Phase 2 null 2013-06-20
    NCT00462280 Precancerous Condition|Stage 0 Melanoma|Stage I Melanoma|Stage II Melanoma Drug: lovastatin|Other: placebo|Procedure: biopsy|Procedure: laboratory biomarker analysis National Cancer Institute (NCI) Phase 2 2007-05-01 2014-10-24

    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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