R1402
Raloxifene hydrochloride
selective estrogen receptor modulator (SERM), solid
别名:
Keoxifene hydrochloride, LY 156758, [6-Hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl][4-[2-(1-piperidinyl)ethoxy]phenyl]methanone hydrochloride
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经验公式（希尔记法）:
C28H27NO4S · HCl
化学文摘社编号:
分子量:
510.04
UNSPSC Code:
51111800
PubChem Substance ID:
NACRES:
NA.77
MDL number:
产品名称
Raloxifene hydrochloride, solid
SMILES string
Cl[H].Oc1ccc(cc1)-c2sc3cc(O)ccc3c2C(=O)c4ccc(OCCN5CCCCC5)cc4
InChI key
BKXVVCILCIUCLG-UHFFFAOYSA-N
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
form
solid
color
light yellow
solubility
DMSO: soluble 28 mg/mL, H2O: insoluble
originator
Eli Lilly
Quality Level
Gene Information
human ... ESR2(2100)
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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.
signalword
Warning
hcodes
Hazard Classifications
Carc. 2 - Repr. 2
存储类别
11 - Combustible Solids
wgk
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Gloves, type N95 (US)
法规信息
监管及禁止进口产品
此项目有
Raloxifene: a selective estrogen receptor modulator (SERM) with multiple target system effects
Muchmore DB
Oncologist, 5(5), 388-392 (2000)
The SERM/SERD bazedoxifene disrupts ESR1 helix 12 to overcome acquired hormone resistance in breast cancer cells
Fanning SW, et al.
eLife, 7, e37161-e37161 (2018)
Rachel K Surowiec et al.
Bone, 173, 116805-116805 (2023-05-18)
Raloxifene (RAL) reduces clinical fracture risk despite modest effects on bone mass and density. This reduction in fracture risk may be due to improved material level-mechanical properties through a non-cell mediated increase in bone hydration. Synthetic salmon calcitonin (CAL) has
Raloxifene
Moen MD, et al.
Drugs (2008)
Oscar Solis et al.
Science advances, 8(48), eadd4150-eadd4150 (2022-12-01)
The severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) spike (S) protein binds angiotensin-converting enzyme 2 as its primary infection mechanism. Interactions between S and endogenous proteins occur after infection but are not well understood. We profiled binding of S against
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