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Raloxifene

Names

[ CAS No. ]:
84449-90-1

[ Name ]:
Raloxifene

[Synonym ]:
[2-(4-Hydroxyphenyl)-6-hydroxybenzo[b]thien-3-yl] [4-[2-(1-piperidinyl)ethoxy]phenyl]methanone
Raloxifeno
[6-Hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl][4-[2-(1-piperidinyl)ethoxy]phenyl]methanone
6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-piperidino-ethoxy)benzoyl]benzo[b]thiophene
[6-hydroxy-2-(4-hydroxyphenyl)-1-benzothiophen-3-yl][4-(2-piperidin-1-ylethoxy)phenyl]methanone
[6-Hydroxy-2-(4-hydroxyphenyl)-1-benzothiophen-3-yl]{4-[2-(1-piperidinyl)ethoxy]phenyl}methanone
[6-Hydroxy-2-(4-hydroxyphenyl)-1-benzothiophen-3-yl]{4-[2-(piperidin-1-yl)ethoxy]phenyl}methanone
UNII-YX9162EO3I
Raloxifenum [Latin]
Raloxifene [INN:BAN]
[6-hydroxy-2-(4-hydroxyphenyl)-1-benzothiophen-3-yl]-[4-(2-piperidin-1-ylethoxy)phenyl]methanone
Raloxifeno [Spanish]
Keoxifene
[3H]-Raloxifene
MFCD00866415
Methanone, [6-hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl][4-[2-(1-piperidinyl)ethoxy]phenyl]-
Methanone, (6-hydroxy-2-(4-hydroxyphenyl)benzo(b)thien-3-yl)(4-(2-(1-piperidinyl)ethoxy)phenyl)-
Raloxifene
[6-hydroxy-2-(4-hydroxyphenyl)-1-benzothien-3-yl]{4-[(2-piperidin-1-ylethyl)oxy]phenyl}methanone
Raloxifenum
[14C]-Raloxifene
Raloxifene HCl

Biological Activity

[Description]:

Raloxifene (Keoxifene) is a benzothiophene-derived selective estrogen receptor modulator (SERM). Raloxifene has estrogen-agonistic effects on bone and lipids and estrogen-antagonistic effects on the breast and uterus. Raloxifene is used for breast cancer and osteoporosis research[1].

[Related Catalog]:

Signaling Pathways >> Others >> Estrogen Receptor/ERR
Research Areas >> Cancer

[Target]

Estrogen receptor


[In Vivo]

Raloxifene (4 mg/kg; intragastrically; daily for 13 weeks) significantly prevents bone loss in ovariectomized (OVX) rats[1]. Animal Model: Female, 12-week-old, Wistar rats (OVX rats)[1] Dosage: 4 mg/kg Administration: Intragastrically; daily for 13 weeks Result: Significantly increased the levels of E2 in OVX rats and significantly decreased the levels of BGP.

[References]

[1]. Khovidhunkit W, et al. Clinical effects of raloxifene hydrochloride in women. Ann Intern Med. 1999;130(5):431-439.

[2]. Xu H, et al. Effect of caffeine on ovariectomy-induced osteoporosis in rats. Biomed Pharmacother. 2019;112:108650.

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
728.2±60.0 °C at 760 mmHg

[ Melting Point ]:
250-253°C

[ Molecular Formula ]:
C28H27NO4S

[ Molecular Weight ]:
473.583

[ Flash Point ]:
394.2±32.9 °C

[ Exact Mass ]:
473.166077

[ PSA ]:
98.24000

[ LogP ]:
6.80

[ Vapour Pressure ]:
0.0±2.5 mmHg at 25°C

[ Index of Refraction ]:
1.666

[ Storage condition ]:
Desiccate at +4°C

[ Water Solubility ]:
DMSO: 28 mg/mL, soluble

Safety Information

[ WGK Germany ]:
3

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Related Compounds