Raloxifene hydrochloride

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

Images & Validation

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Key Properties

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CAS Number	82640-04-8
MW	510.044
Purity	99.97%
Formula	C₂₈H₂₈ClNO₄S
SMILES	Cl.Oc1ccc(cc1)-c1sc2cc(O)ccc2c1C(=O)c1ccc(OCCN2CCCCC2)cc1
Target	Autophagy,Estrogen/progestogen Receptor,Estrogen Receptor/ERR,MAO
Solubility	DMSO:245 mg/mL (480.35 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.92 mM)

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. Read more...
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. Read more...

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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ER, ERR, Estrogen Receptor/ERR, Estrogen Receptor, EstrogenReceptor, inhibit, Inhibitor, Keoxifene, Keoxifene Hydrochloride, Keoxifene hydrochloride, LY 139481, LY 139481 Hydrochloride, LY 156758, LY 156758 Hydrochloride, LY139481, LY-139481, LY139481 Hydrochloride, LY139481 hydrochloride, LY-139481 Hydrochloride, LY156758, LY-156758, LY156758 (Keoxifene) HCl, LY156758 hydrochloride, LY156758 Hydrochloride, LY-156758 Hydrochloride, Autophagy, AO, progestogenReceptor, SERM, progestogen Receptor, Raloxifene HCl, Raloxifene hydrochloride, Raloxifene Hydrochloride, Raloxifene

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Compound Identifiers

PubChem CID

54900 ↗

Key Properties

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No computed properties available.

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