For research use only.
Catalog No.S1227 Synonyms: LY156758 (Keoxifene) HCl
CAS No. 82640-04-8
Raloxifene (LY156758, Keoxifene) HCl a selective and orally active estrogen receptor modulator (SERM), which inhibits human cytosolic aldehyde oxidase-catalyzed phthalazine oxidation activity with IC50 of 5.7 nM.
Selleck's Raloxifene HCl has been cited by 7 publications
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|Description||Raloxifene (LY156758, Keoxifene) HCl a selective and orally active estrogen receptor modulator (SERM), which inhibits human cytosolic aldehyde oxidase-catalyzed phthalazine oxidation activity with IC50 of 5.7 nM.|
|Features||Raloxifene is as effective as tamoxifen in reducing the incidence of breast cancer in postmenopausal women at increased risk.|
Raloxifene, has been demonstrated as a potent uncompetitive inhibitor of human liver aldehyde oxidase-catalyzed oxidation of phthalazine, vanillin, and nicotine-Delta1'(5')-iminium ion, with Ki values of 0.87 nM, 1.2 nM and 1.4 nM. Raloxifene has also been shown to be a noncompetitive inhibitor of an aldehyde oxidase-catalyzed reduction reaction of a hydroxamic acid-containing compound, with a Ki of 51 nM.  Raloxifene activates TGF beta 3 promoter as a full agonist at nanomolar concentrations, and raloxifene inhibits the estrogen response element-containing vitellogenin promoter expression as a pure estrogen antagonist in transient transfection assays. 
Raloxifene restores both bone mineral density and TGF beta 3 messenger RNA expression in the femur to levels measured in intact rats.  Raloxifene (0.1 mg/kg-10 mg/kg, orally for 5 weeks) increases bone mineral density in the distal femur and proximal tibia in ovariectomized (OVX) rat. Raloxifene reduces serum cholesteroloral with ED50 of 0.2 mg/kg in ovariectomized (OVX) rat. Raloxifene diverges dramatically from estrogen in its lack of significant estrogenic effects on uterine tissue.  Raloxifene prevents cancellous osteopenia as well as the changes in radial bone growth, bone resorption, and blood cholesterol, but is less effective in reducing cancellous bone formation and does not prevent uterine atrophy in ovariectomized (OVX) rats.  Raloxifene (3 mg/kg/day) has potent estrogenic activity on bone resorption and serum cholesterol, a lesser effect on bone formation, and minimal activity on uterine wet weight in ovariectomized (OVX) rats. 
-  Obach RS, et al. Drug Metab Dispos, 2004, 32(1), 89-97.
-  Yang NN, et al. Endocrinology, 1996, 137(5), 2075-2084.
-  Black LJ, et al. J Clin Invest, 1994, 93(1), 63-69.
|In vitro||DMSO||100 mg/mL (196.06 mM)|
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|Synonyms||LY156758 (Keoxifene) HCl|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT01573637||Completed||Drug: Raloxifene|Drug: Lactosa (placebo arm)||Negative Symptoms of Schizophrenia in Post-menopausal Women.||Fundació Sant Joan de Déu|Hospital Sant Joan de Deu|Parc Sanitari Sant Joan de Déu|Stanley Medical Research Institute||July 2011||Phase 3|
|NCT01544894||Completed||Drug: Raloxifene|Drug: Strontium ranelate||Postmenopausal Osteoporosis|Compliance||University of Valencia||September 2009||Phase 4|
|NCT00532428||Completed||Drug: Raloxifene|Drug: Placebo||Osteoporosis Post-Menopausal||Eli Lilly and Company||April 2003||Phase 4|
|NCT00532246||Completed||Drug: raloxifene|Drug: Placebo||Osteoporosis Post-Menopausal||Eli Lilly and Company||March 2003||Phase 4|
|NCT00035256||Completed||Drug: teriparatide|Drug: raloxifene HCl|Drug: placebo||Osteoporosis Postmenopausal||Eli Lilly and Company||October 2001||Phase 4|
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