Application in Particular Diseases
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Raloxifene

Application in Particular Diseases
Product Name
Raloxifene
CAS No.
84449-90-1
Chemical Name
Raloxifene
Synonyms
RALOXIFEN;Evista;RALOXAFINE;RALOXIFENE;RALOXIFENE-D7;Raloxifene CRS;Raloxifene USP/EP/BP;Raloxifene hydrochlo;99% Purity Raloxifene;Raloxifene (Evista, RAL) (65)-1 gram
CBNumber
CB1290431
Molecular Formula
C28H27NO4S
Formula Weight
473.58
MOL File
84449-90-1.mol
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Raloxifene Property

Melting point:
250-253°C
Boiling point:
728.2±60.0 °C(Predicted)
Density 
1.289±0.06 g/cm3(Predicted)
storage temp. 
Desiccate at +4°C
solubility 
DMSO: 28 mg/mL, soluble
pka
8.83±0.15(Predicted)
form 
solid
color 
light yellow
Water Solubility 
560μg/L at 25℃
LogP
6.09
CAS DataBase Reference
84449-90-1(CAS DataBase Reference)
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Safety

WGK Germany 
3
HS Code 
29349990
Hazardous Substances Data
84449-90-1(Hazardous Substances Data)
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Danger
Hazard statements

H311Toxic in contact with skin

H360May damage fertility or the unborn child

H411Toxic to aquatic life with long lasting effects

Precautionary statements

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P312Call a POISON CENTER or doctor/physician if you feel unwell.

P322Specific measures (see …on this label).

P361Remove/Take off immediately all contaminated clothing.

P363Wash contaminated clothing before reuse.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

TRC
Product number
R099995
Product name
Raloxifene
Packaging
100mg
Price
$75
Updated
2021/12/16
TRC
Product number
R099995
Product name
Raloxifene
Packaging
1g
Price
$105
Updated
2021/12/16
Usbiological
Product number
464501
Product name
Raloxifene
Packaging
100mg
Price
$355
Updated
2021/12/16
TRC
Product number
R099995
Product name
Raloxifene
Packaging
5g
Price
$470
Updated
2021/12/16
American Custom Chemicals Corporation
Product number
API0003075
Product name
KEOXIFENE
Purity
95.00%
Packaging
50MG
Price
$164.85
Updated
2021/12/16
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Raloxifene Chemical Properties,Usage,Production

Application in Particular Diseases

In Osteoporosis:

  • Raloxifene is an estrogen agonist on bone but an antagonist on the breast and uterus. It is approved for prevention and treatment of postmenopausal osteoporosis. Other estrogen agonists/antagonists may be approved soon (e.g., bazedoxifene, lasofoxifene).
  • Raloxifene decreases vertebral fractures and increases spine and hip BMD, but to a lesser extent than bisphosphonates. After discontinuation, the beneficial effect is lost and bone loss returns to age- or disease-related rates.
  • Raloxifene (like tamoxifen) is associated with decreased breast cancer risk. Raloxifene is associated with decreases in total and low-density lipoprotein cholesterol, neutral effects on high-density lipoprotein cholesterol, but slight increases in triglycerides; no beneficial cardiovascular effects have yet been demonstrated.
  • Raloxifene is well tolerated overall. Hot flushes occur more frequently in women recently finishing menopause or discontinuing estrogen therapy (ET). Endometrial bleeding occurs rarely. Raloxifene is contraindicated in women with an active or past history of venous thromboembolism. Therapy should be stopped if a patient anticipates extended immobility.

Chemical Properties

Light-Yellow Solid

Uses

A nonsteroidal estrogen receptor mixed agonist/antagonist

Uses

Raloxifene is a nonsteroidal, selective estrogen receptor modulator (SERM). Antiosteoporotic.

Indications

Raloxifene (Evista) is a new SERM approved for use in the treatment and prevention of osteoporosis because it has estrogenic activity in bone. Raloxifene is an estrogen antagonist in both breast and endometrial tissues. The estrogenlike properties of raloxifene result in the maintenance of a favorable serum lipid profile (decreased low-density lipoprotein levels with no change in either high-density lipoproteins or triglycerides). Raloxifene is 95% bound to plasma proteins. Absorption of raloxifene is impaired by cholestyramine.

Definition

ChEBI: A member of the class of 1-benzothiophenes that is 1-benzothiophene in which the hydrogens at positions 2, 3, and 6 have been replaced by p-hydroxyphenyl, p-[2-(piperidin-1-yl)ethoxy]benzoyl, and hydroxy groups, respectively.

brand name

Evista (Lilly).

General Description

Raloxifene, [6-hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl][4-[2-(1-piperidinyl)ethoxy]phenyl]methanone (Evista), is a benzothiophene derivativethat differs slightly from the triphenylethyleneSERMs. A key structural difference is the carbonyl “hinge”that connects the modified phenolic side chain to the benzothiophenering system. This hinge is the key structural elementthat leads to the differing actions at the ERs.Raloxifene, unlike tamoxifen and toremifene, has antagonistproperties on the endometrium and breast tissue and agonistproperties on bone and the cardiovascular system. The lackof agonist action on endometrial tissue has been suggestedas a reason for the lack of endometrial cancer associatedwith raloxifene use. Raloxifene is approved for the preventionand treatment of osteoporosis in postmenopausalwomen. It has also been investigated for preventing breastcancer in comparison with tamoxifen. Recent studies indicatesthat it has similar effectiveness to tamoxifen, but has apreferable side effect profile.

Biological Activity

Selective estrogen receptor modulator (SERM) that binds to ER α and ER β , and tissue-dependently activates or blocks estrogen-induced transcription. Acts as an antiestrogen in breast and uterine tissue, but displays estrogen agonist activity in bone. In D12 rat hypothalamic cells, inhibits progesterone receptor induction by estrogen with an IC 50 of 1 nM.

Clinical Use

Raloxifene, the first SERM approved for the prevention of osteoporosis in postmenopausal women, acts as an estrogen agonist on receptors in osteoblasts and osteoclasts but as an antagonist at breast and uterine estrogen receptors.

Raloxifene Preparation Products And Raw materials

Raw materials

Preparation Products

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Raloxifene Suppliers

3B Pharmachem (Wuhan) International Co.,Ltd.
Tel
821-50328103-801 18930552037
Fax
86-21-50328109
Email
3bsc@sina.com
Country
China
ProdList
15848
Advantage
69
LGM Pharma
Tel
1-(800)-881-8210
Fax
615-250-9817
Email
inquiries@lgmpharma.com
Country
United States
ProdList
2127
Advantage
70
Daicel Chiral Technologies (China)CO.,LTD
Tel
021-50460086-9 15921403865
Fax
+86-21-50462321
Email
han_yajun@dctc.daicel.com
Country
China
ProdList
6818
Advantage
65
Syntechem Co.,Ltd
Tel
Fax
E-Mail Inquiry
Email
info@syntechem.com
Country
China
ProdList
12990
Advantage
57
China Langchem Inc.
Tel
021-58956006 15800617331
Fax
021-58956100
Email
sales@langchem.com
Country
China
ProdList
210
Advantage
57
Acorn PharmaTech Co., Ltd.
Tel
025-58395930
Fax
025-5861-9182
Email
sales@acornpharma.com
Country
China
ProdList
982
Advantage
60
Beijing HuaMeiHuLiBiological Chemical
Tel
010-56205725
Fax
010-65763397
Email
waley188@sohu.com
Country
China
ProdList
12338
Advantage
58
Shanghai Topbiochem Technology Co., Ltd
Tel
021-58170097
Email
info@topbiochem.com
Country
China
ProdList
9442
Advantage
58
Nanjing Sunlida Biological Technology Co., Ltd.
Tel
025-57798810
Fax
025-57019371
Email
sales@sunlidabio.com
Country
China
ProdList
3750
Advantage
55
TargetMol Chemicals Inc.
Tel
021-33632979 15002134094
Fax
021-33632979
Email
marketing@targetmol.com
Country
China
ProdList
7934
Advantage
58
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View Lastest Price from Raloxifene manufacturers

Wuhan Biocar Pharmacy Co., Ltd.
Product
Raloxifene 84449-90-1
Price
US $9.90-9.90/g/Bag
Min. Order
10g/Bag
Purity
99.99%HPLC.USP42——Powder、Oil、Pills、Capsules、Tablets,Customized packaging
Supply Ability
100KG/Month
Release date
2022-01-14
Wuhan Senwayer Century Chemical Co.,Ltd
Product
Raloxifene 84449-90-1
Price
US $1330.00/kg
Min. Order
0.1kg
Purity
99% min
Supply Ability
20 tons
Release date
2022-10-13
Anhui Ruihan Technology Co., Ltd
Product
Raloxifene 84449-90-1
Price
US $30.00/kg
Min. Order
1kg
Purity
99%
Supply Ability
1000t/year
Release date
2023-09-06

84449-90-1, RaloxifeneRelated Search:


  • [6-Hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-y1][4-[2-(1-piperidinyl)ethoxy]phenyl]methamone
  • Evista
  • [4-[2-(1-Piperidinyl) Ethoxy] Phenyl]methanone.HCL
  • RALOXAFINE
  • [6-Hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl][4-[2-(1-piperidinyl)ethoxy]phenyl]methanone
  • [6-hydroxy-2-(4-hydroxyphenyl)benzothiophen-3-yl]-[4-[2-(1-piperidyl)ethoxy]phenyl]methanone hydrochloride
  • Methanone, [6-hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl][4-[2-(1-piperidinyl)ethoxy]phenyl]-
  • [6-Hydroxy-2-(4-hydroxyphenyl)benzo[b]thiophen-3-yl][4-[2-(1-piperidinyl)ethoxy]phenyl] ketone
  • [6-Hydroxy-2-(4-hydroxyphenyl)benzo[b]thiophen-3-yl][4-[2-(1-piperidinyl)ethoxy]phenyl]methanone
  • 2-(4-Hydroxyphenyl)-3-[4-(2-piperidinoethoxy)benzoyl]benzo[b]thiophene-6-ol
  • (6-hydroxy-2-(4-hydroxyphenyl)benzo[b]thiophen-3-yl)(4-(2-(piperidin-1-yl)ethoxy)phenyl)Methanone
  • [6-Hydroxy-2-(4-hydroxyphenyl)benzothien-3-yl][4-[2-(1-piperidinyl)ethoxy]phenyl]-methanone
  • (6-Hydroxy-2-(4-hydroxyphenyl)benzo[b]thiophen-3-yl)(4-(2-(piperidin-1-yl)ethoxy)phenyl)methan
  • RALOXIFEN
  • RALOXIFENE
  • Raloxifene CRS
  • Raloxifene for peak identification CRS
  • Raloxifene USP/EP/BP
  • 99% Purity Raloxifene
  • Raloxifene hydrochlo
  • RALOXIFENE-D7
  • Raloxifene (Evista, RAL) (65)-1 gram
  • 84449-90-1
  • C28H28ClNO4S
  • C28H27NO4S
  • BioChemical
  • Cell Signaling and Neuroscience
  • Cell Biology
  • Estrogen
  • Cytokines, Growth Factors and Hormones
  • Hormones
  • Steroid Hormones
  • Raloxifene
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
  • Pharmaceutical intermediate