Raloxifene HCl

盐酸雷洛昔芬,LY156758 HCl,Keoxifene hydrochloride

Raloxifene hydrochloride 是第二代雌激素受体拮抗剂。

目录号
EY1446
EY1446
纯度
99.37%
99.37%
规格
50 mg
100 mg
原价
690
1060
售价
690
1060
库存
现货
现货
订购
订购
订购
订购
订购
订购
  • 生物活性

    Raloxifene is an estrogen antagonist, which inhibits human cytosolic aldehyde oxidase-catalyzed phthalazine oxidation activity with IC50 of 5.7 nM.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

  • 动物实验

    10mg/kg 口服

  • 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] Obach RS, et al. Drug Metab Dispos, 2004, 32(1), 89-97.
    [2] Fitzpatrick et al (1999) Effect of estrogen agonists and antagonists on induction of progesterone receptor in a rat hypothalamic cell line. Endocrinology 140 3928.
    [3] Hibner et al (2004) Effects of raloxifene hydrochloride on endometrial cancer cells in vitro. Gynecologic Oncol. 93 642.
    [4] Todorova (2011) Tamoxifen and raloxifene suppress the proliferation of estrogen receptor-negative cells through inhibition of glutamine uptake. Cancer Chemother. Pharmacol. 67 285.

    分子式
    C28H28ClNO4S
    分子量
    510.04
    CAS号
    82640-04-8
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    50 mM
    Water
    Insoluble
    Ethanol
    <1 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
    NCT00035256 Osteoporosis, Postmenopausal Drug: teriparatide|Drug: raloxifene HCl|Drug: placebo Eli Lilly and Company Phase 4 2001-10-01 2007-05-11
    NCT00670319 Osteoporosis, Postmenopausal Drug: Raloxifene HCL|Drug: Raloxifene HCL|Drug: Placebo Eli Lilly and Company Phase 3 1994-11-01 2008-04-30
    NCT00368459 Alzheimer Disease Drug: raloxifene|Drug: Placebo Stanford University|Kaiser Permanente|Indiana University|Southern Illinois University Phase 2 2006-08-01 2015-03-20
    NCT00532246 Osteoporosis, Post-Menopausal Drug: raloxifene|Drug: Placebo Eli Lilly and Company Phase 4 2003-03-01 2007-09-18
    NCT02982083 Rheumatoid Arthritis Drug: Raloxifene hydrochloride|Drug: Placebo Oral Tablet Sara Saeidi Shahri|Mashhad University of Medical Sciences 2016-12-01 2016-12-02
    NCT01544894 Postmenopausal Osteoporosis|Compliance Drug: Raloxifene|Drug: Strontium ranelate University of Valencia Phase 4 2009-09-01 2012-08-31
    NCT03043820 Schizophrenia|Schizoaffective Disorder|Schizophreniform Disorder|Psychosis NOS Drug: Raloxifene|Drug: Placebo Iris Sommer|Julius Center|Rudolf Magnus Institute 鈥?University of Utrecht|GGZ Eindhoven|Academisch Medisch Centrum - Universiteit van Amsterdam (AMC-UvA)|GGZ Centraal|Altrecht GGZ|Reinier van Arkel Group|Ziekenhuis Netwerk Antwerpen (ZNA)|UMC Utrecht Phase 3 2016-08-01 2017-02-02
    NCT00532428 Osteoporosis, Post-Menopausal Drug: Raloxifene|Drug: Raloxifene|Drug: Placebo Eli Lilly and Company Phase 4 2003-04-01 2007-09-18
    NCT00427700 Polycystic Ovary Syndrome Drug: clomiphene citrate|Drug: raloxifene Hospital de Clinicas de Porto Alegre Phase 3 2008-08-01 2016-08-15
    NCT00687102 Cognition|Aging Drug: tamoxifen|Drug: raloxifene Wake Forest University|National Institute on Aging (NIA)|Wake Forest University Health Sciences Phase 3 2001-10-01 2011-08-03
    NCT00200174 Breast Cancer Drug: Raloxifene followed by combination therapy|Drug: Exemestane followed by combination therapy Memorial Sloan Kettering Cancer Center|Pharmacia 1999-07-01 2015-12-21
    NCT00790101 Osteoporosis, Postmenopausal Drug: Risedronate|Drug: Raloxifene|Other: Placebo Sanofi Phase 4 2004-06-01 2011-01-10
    NCT01607320 Polycystic Ovarian Syndrome Drug: Raloxifene|Drug: Clomiphene Bruce Lessey|Greenville Health System 2012-06-01 2015-05-12
    NCT01280305 Schizophrenia|Schizoaffective Disorder Drug: raloxifene|Drug: placebo Sheba Medical Center Phase 3 2011-03-01 2011-01-19
    NCT00332553 Vasomotor Symptoms|Endometrial Safety Drug: Raloxifene|Drug: medroxyprogesterone acetate|Drug: estrogen|Drug: 17 beta estradiol Eli Lilly and Company Phase 2 2002-02-01 2007-05-11
    NCT00191425 Osteoporosis, Postmenopausal Drug: Teriparatide|Drug: Raloxifene Eli Lilly and Company Phase 4 2002-08-01 2007-07-12
    NCT00383422 Osteoporosis, Postmenopausal Drug: Arzoxifene|Drug: Raloxifene Eli Lilly and Company Phase 3 2006-10-01 2010-01-26
    NCT00163137 Osteoporosis Drug: lasofoxifene|Drug: raloxifene|Drug: Placebo Ligand Pharmaceuticals Phase 3 2003-05-01 2011-08-10
    NCT00371956 Osteoporosis Drug: raloxifene|Drug: placebo Tuen Mun Hospital|Eli Lilly and Company Phase 4 2006-09-01 2010-09-15
    NCT01050842 Prostate Cancer|Adenocarcinoma of the Prostate|Hormone-resistant Prostate Cancer|Stage IV Prostate Cancer Drug: bicalutamide|Drug: raloxifene|Procedure: quality-of-life assessment Mayo Clinic Early Phase 1 2010-02-01 2017-03-21

    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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