Raloxifene HCl , ≥98% , 82640-04-8

Synonym(s):
[6-Hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl][4-[2-(1-piperidinyl)ethoxy]phenyl]methanone hydrochloride;Keoxifene hydrochloride;LY 156758;Raloxifene hydrochloride

CAS NO.：82640-04-8

Empirical Formula: C28H28ClNO4S

Molecular Weight: 510.04

MDL number: MFCD01938233

EINECS: 639-789-7

PRODUCT Properties

• Melting point: 250-253°C
• storage temp.: 2-8°C
• solubility: DMSO: 28 mg/mL, soluble
• form: solid
• color: light yellow
• λmax: 286nm(lit.)
• Merck: 14,8098
• BCS Class: 2
• InChIKey: BKXVVCILCIUCLG-UHFFFAOYSA-N
• SMILES: C1(C(=O)C2C=CC(OCCN3CCCCC3)=CC=2)C2C=CC(O)=CC=2SC=1C1C=CC(O)=CC=1.Cl

Description and Uses

Raloxifene was launched as Evista in the US for the prevention of postmenopausal osteoporosis. It is noteworthy that this molecule was formerly under development as keoxifene for breast cancer and prostatic hypertrophy. Raloxifene can be prepared by acylation of 6-methoxy-2-(4-methoxyphenyl) benzothiophene followed by simultaneous demethylation of both methoxy groups. Raloxifen is a selective estrogen receptor modulator, exerting antiestrogenic action on certain tissues (breast) and also estrogenic action on bone metabolism or serum lipids. In normal early postmenopausal women, 200 mg daily produced a trend towards suppression of estrogen effects. Raloxifen impeded bone loss in osteoporosis. A two-year study in postmenopausal women with an increased risk for osteoporosis showed that Raloxifen markedly prevented non-traumatic vertebral fractures. Results of several clinical studies demonstrated that Raloxifen appreciably reduced the risk of developing breast cancer. Moreover, it had favourable effect on lipid profiles without having the potential side-effects of estrogen-based therapies. Several extensions for different uses of this molecule are planned, for example growth disorder, obesity, colon tumor and skin atrophy. No serious drug-related events have been reported in the limited number of clinical trials.

Labeled Raloxifene, intended for use as an internal standard for the quantification of Raloxifene by GC- or LC-mass spectrometry.

Safety

• Symbol(GHS): GHS08
• Signal word: Warning
• Hazard statements: H351-H361d
• Precautionary statements: P201-P202-P280-P308+P313-P405-P501
• Hazard Codes: Xi
• Risk Statements: 36/37/38
• Safety Statements: 22-24/25
• WGK Germany: 3
• RTECS: PC4956925
• HS Code: 2934990002