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Raloxifene HCl

SKU: orb1308226
FeaturedFeatured Product

Description

Raloxifene hydrochloride is a selective estrogen receptor modulator (SERM) used in research to study osteoporosis prevention. It exhibits tissue-specific estrogenic activity on bone and anti-estrogenic effects on breast and uterine tissue, making it a key tool for in vitro and in vivo studies of hormone-responsive cancers and metabolic diseases.

Research Area

Cell Biology, Metabolism Research, Neuroscience, Pharmacology & Drug Discovery

Images & Validation

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Raloxifene HCl

Key Properties

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CAS Number82640-04-8
MW510.0
Purity>98%
FormulaC28H27NO4S • HCl
SMILESCl.Oc1ccc(cc1)-c1sc2cc(O)ccc2c1C(=O)c1ccc(OCCN2CCCCC2)cc1
TargetTranscription factor
SolubilitySoluble in DMSO (up to 15 mg/ml)

Bioactivity

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Target IC50
ER:5.7 nM
In Vivo
Raloxifene is a non-competitive inhibitor of aldehyde oxidase (with a Ki of 51 nM), targeting the enzyme's reduction reaction of compounds containing isohydroxystearic acid. It has been proven to effectively inhibit the human liver aldehyde oxidase-catalyzed oxidation of phthalazine, vanillin, and nicotine-δ1' (5')- iminium with Ki values of 0.87 nM, 1.2 nM, and 1.4 nM, respectively. Additionally, Raloxifene acts as a full agonist at nanomolar concentrations, activating the TGFβ 3 promoter, and serves as a pure estrogen antagonist in transient transfection assays by inhibiting the expression of vitellogenin promoter with estrogen response elements.
In Vitro
Raloxifene significantly differs from estrogen due to its lack of substantial estrogenic effects on uterine tissues. In rat femurs, Raloxifene rebuilds bone mineral density and the expression of TGF beta 3 mRNA. Oral administration of 0.1 mg/kg to 10 mg/kg of Raloxifene for 5 weeks increases the density of femurs and tibias in ovariectomized rats. With an ED50 of 0.2 mg/kg, Raloxifene reduces serum cholesterol levels in ovariectomized (OVX) rats. In ovariectomized rats, Raloxifene blocks the deterioration of bone quality and growth changes, bone remodeling, and serum cholesterol content, albeit with lesser effects on reducing bone formation and unable to prevent uterine atrophy.

Storage & Handling

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Storage-20°C
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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Keoxifene; LY156758

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Quality Guarantee

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Compound Identifiers

PubChem CID
54900 ↗

Key Properties

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No computed properties available.

Protocol Information

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50 mg
$ 170.00
250 mg
$ 290.00
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