LY 156758
Raloxifene hydrochloride
CAS: 82640-04-8
Molecular Formula: C28H28ClNO4S
LY 156758 - Names and Identifiers
LY 156758 - Physico-chemical Properties
| Molecular Formula | C28H28ClNO4S |
| Molar Mass | 510.04 |
| Density | 1.285g/cm3 |
| Melting Point | 250-253°C |
| Boling Point | 687.5°C at 760 mmHg |
| Flash Point | 369.6°C |
| Solubility | DMSO: 28mg/mL, soluble |
| Vapor Presure | 1.56E-19mmHg at 25°C |
| Appearance | solid |
| Color | light yellow |
| Maximum wavelength(λmax) | ['286nm(lit.)'] |
| Merck | 14,8098 |
| Storage Condition | 2-8°C |
| Refractive Index | 1.654 |
| In vitro study | Raloxifene has been shown to be a potent, non-competitive inhibitor of human liver aldehyde dehydrogenase-catalyzed oxidation of phthalazine, vanillin, and nicotine-delta '(5') -imine ions, the Ki values were 0.87 nM, 1.2 nM and 1.4 nM, respectively. Raloxifene is also a noncompetitive inhibitor, inhibiting aldehyde dehydrogenase-catalyzed reduction of hydroxamic acid-containing compounds with an Ki value of 51 nM. Raloxifene activates the TGF β 3 Promoter as a full agonist at nanomolar concentrations, and in transient transfection experiments raloxifene inhibits the expression of estrogen-responsive elements containing the vitellogenin Promoter as a pure estrogen antagonist. |
| In vivo study | In rat femurs, Raloxifene reconstructs bone mineral density and TGF beta 3 mRNA expression. Raloxifene (0.1 mg/kg -10 mg/kg orally for 5 weeks) increased femur and tibia density in ovariectomized rats. In ovariectomized rats, Raloxifene reduces serum cholesterol levels to an ED50 of 0.2 mg/kg. Raloxifene causes a marked lack of estrogenic action in uterine tissue. In ovariectomized rats, Raloxifene blocked osteopenia and changes in bone growth, bone remodeling, and blood cholesterol content, but was less effective in reducing bone formation and did not prevent uterine atrophy. |
LY 156758 - Risk and Safety
| Hazard Symbols | Xi - Irritant |
| Risk Codes | 36/37/38 - Irritating to eyes, respiratory system and skin. |
| Safety Description | S22 - Do not breathe dust. S24/25 - Avoid contact with skin and eyes. |
| WGK Germany | 3 |
| RTECS | PC4956925 |
| HS Code | 2934990002 |
LY 156758 - Nature
Open Data Verified Data
crystallized from methanol-water, melting point 258 °c. UV maximum absorption (ethanol):286nm(e32800)a
Last Update：2024-01-02 23:10:35
LY 156758 - Use
Open Data Verified Data
It was developed by the U. S. Lily and company and was launched in the United States in January 1998. Estrogen receptor modulators, in the uterus and breast tissue showed antagonistic estrogen effect, inhibition of mammary epithelial and endometrial hyperplasia. In the aspect of bone lipid metabolism showed Excitatory effect, with the role of estrogen. The combination of raloxifene and calcium preparations can prevent bone loss, maintain bone density and reduce blood wax.
Last Update：2022-01-01 09:24:22
