Raloxifene HCl 82640-04-8

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Molecular Weight:

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

Biological Activity

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.

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Product Categories : Endocrinology & Hormones > Estrogen/progestogen Receptor Inhibitor