Raloxifene HCl

SKU: orb1308226

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

Key Properties

• CAS Number: 82640-04-8
• MW: 510.0
• Purity: >98%
• Formula: C₂₈H₂₇NO₄S • HCl
• SMILES: Cl.Oc1ccc(cc1)-c1sc2cc(O)ccc2c1C(=O)c1ccc(OCCN2CCCCC2)cc1
• Target: Transcription factor
• Solubility: Soluble in DMSO (up to 15 mg/ml)

Bioactivity

• 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.
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• 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Keoxifene; LY156758

Compound Identifiers

PubChem CID

54900