Home Endocrinology & Hormones Estrogen/progestogen Receptor modulator Raloxifene HCl For research use only.

Raloxifene HCl

Synonyms: LY156758 (Keoxifene) HCl

Raloxifene (LY156758, Keoxifene) HCl is 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.

Raloxifene HCl Chemical Structure

Raloxifene HCl Chemical Structure

CAS No. 82640-04-8

Purity & Quality Control

Raloxifene HCl Related Products

Signaling Pathway

Estrogen/progestogen Receptor Signaling Pathways

Estrogen/progestogen Receptor Signaling Pathway

Biological Activity

Description Raloxifene (LY156758, Keoxifene) HCl is 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.
Targets
ER [1]
(Cell-free assay)
5.7 nM
In vitro
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]
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-STAT3 / STAT3 / Survivin / Bcl-2 / Bcl-xl RhoA / Rock I / Rock II / p-MLC / MLC 28430601
Growth inhibition assay Cell viability 28430601
In Vivo
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]
Animal Research Animal Models ovariectomized (OVX) rat
Dosages 10 mg/kg
Administration Orally
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01973738 Unknown status
Selective Estrogen Receptor Modulator
Toshihiko Kono|Tomidahama Hospital
 January 2012 --
NCT02977949 Unknown status
Selective Estrogen Receptor Modulator (SERM)
Toshihiko Kono|Tomidahama Hospital
 January 2012 --
NCT01573637 Completed
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

Chemical Information & Solubility

Molecular Weight 510.04 Formula

C28H27NO4S.HCl
CAS No. 82640-04-8 SDF Download Raloxifene HCl SDF
Smiles C1CCN(CC1)CCOC2=CC=C(C=C2)C(=O)C3=C(SC4=C3C=CC(=C4)O)C5=CC=C(C=C5)O.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (196.06 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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