Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Raloxifene hydrochloride (LY156758 hydrochloride) is a second generation selective estrogen receptor modulator (SERM) used to prevent osteoporosis in postmenopausal women. It has estrogen agonist effects on bone and cholesterol metabolism but behaves as a complete estrogen antagonist on mammary gland and uterine tissue.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
25 mg | In stock | $ 38.00 | |
50 mg | In stock | $ 54.00 | |
100 mg | In stock | $ 81.00 | |
200 mg | In stock | $ 121.00 | |
500 mg | In stock | $ 196.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 58.00 |
Description | Raloxifene hydrochloride (LY156758 hydrochloride) is a second generation selective estrogen receptor modulator (SERM) used to prevent osteoporosis in postmenopausal women. It has estrogen agonist effects on bone and cholesterol metabolism but behaves as a complete estrogen antagonist on mammary gland and uterine tissue. |
Targets&IC50 | ER:5.7 nM |
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. |
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. |
Synonyms | LY156758 hydrochloride, Raloxifene HCl, LY139481 hydrochloride, Keoxifene hydrochloride, LY156758 (Keoxifene) HCl |
Molecular Weight | 510.044 |
Formula | C28H28ClNO4S |
CAS No. | 82640-04-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 25.5 mg/mL (50 mM)
You can also refer to dose conversion for different animals. More
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Raloxifene hydrochloride 82640-04-8 Autophagy Endocrinology/Hormones Metabolism Neuroscience Others MAO Estrogen/progestogen Receptor Estrogen Receptor/ERR LY156758 hydrochloride LY 139481 Keoxifene Hydrochloride Inhibitor Raloxifene LY-139481 Hydrochloride LY156758 Hydrochloride Keoxifene LY 156758 LY-139481 Raloxifene HCl LY139481 LY-156758 LY139481 Hydrochloride LY 139481 Hydrochloride LY156758 LY139481 hydrochloride LY-156758 Hydrochloride inhibit LY 156758 Hydrochloride Raloxifene Hydrochloride Keoxifene hydrochloride LY156758 (Keoxifene) HCl inhibitor