Raloxifene hydrochloride 是第二代雌激素受体拮抗剂。
Raloxifene is an estrogen antagonist, which inhibits human cytosolic aldehyde oxidase-catalyzed phthalazine oxidation activity with IC50 of 5.7 nM.
10mg/kg 口服
动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km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。
[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
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。
相关化合物库
使用AMQUAR产品发表文献后请联系我们