R1402

Raloxifene hydrochloride

selective estrogen receptor modulator (SERM), solid

• Synonym(s): Keoxifene hydrochloride, LY 156758, [6-Hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl][4-[2-(1-piperidinyl)ethoxy]phenyl]methanone hydrochloride
• Empirical Formula (Hill Notation): C₂₈H₂₇NO₄S · HCl
• CAS Number: 82640-04-8
• Molecular Weight: 510.04
• UNSPSC Code: 51111800
• PubChem Substance ID: 24278673
• NACRES: NA.77
• MDL number: MFCD01938233
• Form: solid

Properties

• Product Name: Raloxifene hydrochloride, solid
• form: solid
• Quality Segment: 100
• color: light yellow
• solubility: DMSO: soluble 28 mg/mL, H₂O: insoluble
• originator: Eli Lilly
• SMILES string: Cl[H].Oc1ccc(cc1)-c2sc3cc(O)ccc3c2C(=O)c4ccc(OCCN5CCCCC5)cc4
• InChI: 1S/C28H27NO4S.ClH/c30-21-8-4-20(5-9-21)28-26(24-13-10-22(31)18-25(24)34-28)27(32)19-6-11-23(12-7-19)33-17-16-29-14-2-1-3-15-29;/h4-13,18,30-31H,1-3,14-17H2;1H
• InChI key: BKXVVCILCIUCLG-UHFFFAOYSA-N
• Gene Information: human ... ESR2(2100)

Description

Application

Raloxifene hydrochloride has been used:

• as a competitive inhibitors for estrogen receptor α in breast cancer cells
• as an anti-resorptive agents to test its effect on improving bone mineral density (BMD) in six-month-old female ovariectomized rats
• to test effect on viability of esophageal adenocarcinoma cells

Biochem/physiol Actions

Raloxifene is a selective estrogen receptor modulator (SERM); acts as an anti-estrogen in both breast and uterine tissue while being estrogenic in bone. May have efficacy against estrogen-sensitive cancers.

Raloxifene is benzothiophene compound and is used in treating postmenopausal osteoporosis It comparatively induces lesser risk in developing thromboembolic events and cataracts compared to tamoxifen. Raloxifene also interacts with estrogen receptors and plasma proteins.

Features and Benefits

This compound is featured on the Nuclear Receptors (Steroids) page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

This compound was developed by Eli Lilly. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Safety Information

• pictograms: GHS08
• signalword: Warning
• hcodes: H351,H361d
• pcodes: P201 - P202 - P280 - P308 + P313 - P405 - P501
• Hazard Classifications: Carc. 2 - Repr. 2
• Storage Class: 11 - Combustible Solids
• wgk: WGK 2
• flash_point_f: Not applicable
• flash_point_c: Not applicable
• ppe: Eyeshields, Gloves, type N95 (US)