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Key Documents

R1402

Sigma-Aldrich

Raloxifene hydrochloride

solid

Sinônimo(s):

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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About This Item

Fórmula empírica (Notação de Hill):
C28H27NO4S · HCl
Número CAS:
Peso molecular:
510.04
Número MDL:
Código UNSPSC:
51111800
ID de substância PubChem:
NACRES:
NA.77

forma

solid

Nível de qualidade

cor

light yellow

solubilidade

DMSO: soluble 28 mg/mL
H2O: insoluble

originador

Eli Lilly

cadeia de caracteres SMILES

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

chave InChI

BKXVVCILCIUCLG-UHFFFAOYSA-N

Informações sobre genes

human ... ESR2(2100)

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Aplicação

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

Ações bioquímicas/fisiológicas

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.
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.

Características e benefícios

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.

Pictogramas

Health hazard

Palavra indicadora

Warning

Frases de perigo

Classificações de perigo

Carc. 2 - Repr. 2

Código de classe de armazenamento

11 - Combustible Solids

Classe de risco de água (WGK)

WGK 2

Ponto de fulgor (°F)

Not applicable

Ponto de fulgor (°C)

Not applicable

Equipamento de proteção individual

Eyeshields, Gloves, type N95 (US)


Certificados de análise (COA)

Busque Certificados de análise (COA) digitando o Número do Lote do produto. Os números de lote e remessa podem ser encontrados no rótulo de um produto após a palavra “Lot” ou “Batch”.

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Raloxifene: a selective estrogen receptor modulator (SERM) with multiple target system effects
Muchmore DB
Oncologist, 5(5), 388-392 (2000)
Effect of osteoporosis treatment agents on the cortical bone osteocyte microenvironment in adult estrogen-deficient, osteopenic rats
Stern AR, et al.
BoneKEy reports, 8, 115-124 (2018)
Raloxifene
Moen MD, et al.
Drugs (2008)
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)
Effects of chemotherapy agents on Sphingosine-1-Phosphate receptors expression in MCF-7 mammary cancer cells
Ghosal P, et al.
Biomedicine and Pharmacotherapy, 81, 218-224 (2016)

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