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Raloxifene hydrochloride

Raloxifene hydrochloride structure

CAS No:
82640-04-8
Formula:
C28H27NO4S.ClH
Chemical Name:
Raloxifene hydrochloride
Synonyms:
Methanone,[6-hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl][4-[2-(1-piperidinyl)ethoxy]phenyl]-,hydrochloride (1:1);Methanone,[6-hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl][4-[2-(1-piperidinyl)ethoxy]phenyl]-,hydrochloride;LY 156758;Raloxifene hydrochloride;Evista;Keoxifene hydrochloride;Fiona;Bonebay;Reloxafine;Bontact;Ralofen;Ralista;2-(4-Hydroxyphenyl)-3-[4-[2-(piperidin-1-yl)ethoxy]benzoyl]-1-benzothiophen-6-ol hydrochloride;Optruma
Categories:
Biochemical Engineering > Inhibitors

Description

Raloxifene hydrochloride(LY156758 hydrochloride) is a second generation selective estrogen receptor antagonist.Target: Estrogen receptorApproved: September 14, 2007Raloxifene activates TGF beta 3 promoter as a full agonist at nanomolar concentrations, and raloxifene inhibits the estrogen response element-containing vitellogenin promoter expression as a pure estrogen antagonist in transient transfection assays [1]. Raloxifene, has been demonstrated as a potent uncompetitive inhibitor of h

Raloxifene hydrochloride is a hydrochloride salt resulting from the reaction of equimolar amounts of raloxifene and hydrogen chloride. It has a role as a bone density conservation agent, an estrogen antagonist and an estrogen receptor modulator. It contains a raloxifene(1+).|Raloxifene Hydrochloride is the hydrochloride salt form of raloxifene, a selective benzothiophene estrogen receptor modulator (SERM) with lipid lowering effects and activity against osteoporosis. Raloxifene hydrochloride specifically binds to estrogen receptors in responsive tissue, including liver, bone, breast, and endometrium. The resulting ligand-receptor complex is translocated to the nucleus where, depending on the tissue type, it promotes or suppresses the transcription of estrogen-regulated genes, thereby exerting its agonistic or antagonistic effects. This agent functions as an estrogen agonist in lipid metabolism, thereby decreasing total and LDL cholesterol levels. In tissue like bone, it decreases bone resorption and bone turnover and increases bone mineral density. Raloxifene hydrochloride acts as an estrogen antagonist in uterine and breast tissue. This agent also exerts an anti-proliferative effect on estrogen-sensitive breast cancer.|A second generation selective estrogen receptor modulator (SERM) used to prevent osteoporosis in postmenopausal women. It has estrogen agonist effects on bone and cholesterol metabolism but behaves as a complete estrogen antagonist on mammary gland and uterine tissue.

Raloxifene hydrochloride Basic Attributes

Molecular Weight：

510.04

Exact Mass：

509.142761

EC Number：

1308068-626-2

UNII：

4F86W47BR6

NSC Number：

759285|706725

DSSTox ID：

DTXSID1034181

NCI Thesaurus Code：

C1762

ATC Code：

G03XC01

HScode：

2934990002

Characteristics

PSA：

98.24000

XLogP3：

6.81510

Appearance：

light yellow solid

Density：

1.285g/cm3

Melting Point：

258 °C

Boiling Point：

728.2ºC at 760 mmHg

Flash Point：

394.2ºC

Refractive Index：

1.654

Water Solubility：

DMSO: 28 mg/mL, soluble

Storage Conditions：

-20°C Freezer

Collision Cross Section：

213.4 Å² [M+H]+ [CCS Type: TW, Method: calibrated with polyalanine and drug standards]

Safety Information

Transport codes：

NONH for all modes of transport

wgk germany：

hazard class code：

36/37/38

safety instructions：

22-24/25

RTECS Number：

PC4956925

Marks：

Precautionary statement(s)：

P201, P202, P273, P281, P308+P313, P391, P405, P501

Hazard Statements：

H351

GHS Classification：

|Danger|H351 (83.58%): Suspected of causing cancer [Warning Carcinogenicity]|P201, P202, P273, P281, P308+P313, P391, P405, and P501|Aggregated GHS information provided by 67 companies from 15 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Drug Information

Drug Indication：

Optruma is indicated for the treatment and prevention of osteoporosis in post-menopausal women. A significant reduction in the incidence of vertebral, but not hip fractures has been demonstrated. When determining the choice of Optruma or other therapies, including oestrogens, for an individual postmenopausal woman, consideration should be given to menopausal symptoms, effects on uterine and breast tissues, and cardiovascular risks and benefits (see section 5.1).|Evista is indicated for the treatment and prevention of osteoporosis in post-menopausal women. A significant reduction in the incidence of vertebral, but not hip fractures has been demonstrated. When determining the choice of Evista or other therapies, including oestrogens, for an individual postmenopausal woman, consideration should be given to menopausal symptoms, effects on uterine and breast tissues, and cardiovascular risks and benefits.|Raloxifene is indicated for the treatment and prevention of osteoporosis in postmenopausal women. A significant reduction in the incidence of vertebral, but not hip fractures has been demonstrated.When determining the choice of raloxifene or other therapies, including oestrogens, for an individual postmenopausal woman, consideration should be given to menopausal symptoms, effects on uterine and breast tissues, and cardiovascular risks and benefits.|Drug: Raloxifenehydrochloride

MeSH：

A structurally diverse group of compounds distinguished from ESTROGENS by their ability to bind and activate ESTROGEN RECEPTORS but act as either an agonist or antagonist depending on the tissue type and hormonal milieu. They are classified as either first generation because they demonstrate estrogen agonist properties in the ENDOMETRIUM or second generation based on their patterns of tissue specificity. (Horm Res 1997;48:155-63) (See all compounds classified as Selective Estrogen Receptor Modulators.)|Agents that inhibit BONE RESORPTION and/or favor BONE MINERALIZATION and BONE REGENERATION. They are used to heal BONE FRACTURES and to treat METABOLIC BONE DISEASES such as OSTEOPOROSIS. (See all compounds classified as Bone Density Conservation Agents.)|Compounds which inhibit or antagonize the action or biosynthesis of estrogenic compounds. (See all compounds classified as Estrogen Antagonists.)

MeSH Entry Terms：

Evista

Raloxifene hydrochloride Use and Manufacturing

Uses

A nonsteroidal, selective estrogen receptor modulator (SERM). Antiosteoporotic.

Use Classification：

Human drugs -> Optruma -> EMA Drug Category|Sex hormones and modulators of the genital system -> Human pharmacotherapeutic group|Human drugs -> Evista -> EMA Drug Category|Human drugs -> Raloxifene Teva -> EMA Drug Category|Human drugs -> Rare disease (orphan)|Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients

Computed Properties

Molecular Weight:510.0
Hydrogen Bond Donor Count:3
Hydrogen Bond Acceptor Count:6
Rotatable Bond Count:7
Exact Mass:509.1427572
Monoisotopic Mass:509.1427572
Topological Polar Surface Area:98.2
Heavy Atom Count:35
Complexity:655
Covalently-Bonded Unit Count:2
Compound Is Canonicalized:Yes

Drug Function and Efficacy

Raloxifene is a selective estrogen receptor modulator that activates certain estrogen pathways and blocks other pathways after binding to estrogen receptors. Raloxifene reduces bone reabsorption and can reduce biochemical indicators of bone turnover to the premenopausal range. Raloxifene can also affect lipid metabolism, reducing total and LDL cholesterol levels, but does not increase triglyceride levels and has no effect on total HDL levels.

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Raloxifene Hydrochloride
Manufacturer	Jiangsu Hengrui Pharmaceuticals Co., Ltd.

Raloxifene Hydrochloride Tablets
Ingredients	The main ingredient of this product is raloxifene hydrochloride, and its chemical name is: 2-(4-hydroxyphenyl)-3-{4-[2-(1-piperidinyl)ethoxy]benzoyl}-6-hydroxybenzo[b]thiophenol hydrochloride.
Indication	Concomitant ingestion of calcium carbonate or antacids containing aluminum and magnesium hydroxide has no effect on systemic raloxifene. Concomitant administration of raloxifene and warfarin does not alter the pharmacokinetics of either compound. However, it has been found to slightly reduce the prothrombin time, so monitoring of the prothrombin time is necessary when raloxifene is co-administered with warfarin or other coumarin derivatives. An effect on the prothrombin time may occur in patients already receiving coumarin anticoagulation several weeks after initiation of raloxifene therapy.
Specifications	60mg
Manufacturer	Jiangsu Hengrui Pharmaceuticals Co., Ltd.

Raloxifene Hydrochloride Tablets
Specifications	60mg (calculated as C28H27NO4S·HCl)

See More Related Drugs

Registered Holders

GLOCHEM INDUSTRIES PRIVATE LTD

United States
Active
APITORIA PHARMA PRIVATE LTD

United States
Active
Cambrex Profarmaco Milano S.r.l.

Japan
Active

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