Raloxifene HCl

Catalog No.S1227 Synonyms: LY156758 (Keoxifene) HCl

Raloxifene HCl Chemical Structure

Molecular Weight(MW): 510.04

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

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In DMSO USD 160 In stock
USD 97 In stock
USD 170 In stock
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  • J Med Chem 2014 57(3), 632-41. Raloxifene HCl purchased from Selleck.

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Choose Selective Estrogen/progestogen Receptor Inhibitors

Biological Activity

Description Raloxifene is an estrogen antagonist, 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.
Targets
ER [1]
(Cell-free assay)
5.7 nM
In vitro

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. [1] 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. [2]

In vivo Raloxifene restores both bone mineral density and TGF beta 3 messenger RNA expression in the femur to levels measured in intact rats. [2] 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. [3] 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. [4] 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. [5]

Protocol

Animal Research:

[3]

+ Expand
  • Animal Models: ovariectomized (OVX) rat
  • Formulation: 1.5% carboxymethylcellulose
  • Dosages: 10 mg/kg
  • Administration: Orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (196.06 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order:
1% methylcellulose
For best results, use promptly after mixing.
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 510.04
Formula

C28H27NO4S.HCl

CAS No. 82640-04-8
Storage powder
Synonyms LY156758 (Keoxifene) HCl

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03010267 Not yet recruiting Healthy Alvogen Korea January 2017 Phase 1
NCT02982083 Not yet recruiting Rheumatoid Arthritis Sara Saeidi Shahri|Mashhad University of Medical Sciences December 2016 --
NCT03006003 Not yet recruiting Depressive Syndrome Taichung Veterans General Hospital December 2016 Phase 4
NCT03043820 Recruiting Schizophrenia|Schizoaffective Disorder|Schizophreniform Disorder|Psychosis NOS Iris Sommer|Julius Center|Rudolf Magnus Institute – 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 August 2016 Phase 3
NCT02762643 Completed Healthy Alvogen Korea May 2016 Phase 1
NCT02654093 Completed Healthy Alvogen Korea January 2016 Phase 1

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Estrogen/progestogen Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID