Raloxifene hydrochloride

Bezeichnung:Raloxifene hydrochloride

CAS-Nr82640-04-8

Englisch Name:Raloxifene hydrochloride

CBNumberCB6302366

SummenformelC28H28ClNO4S

Molgewicht510.04

MOL-Datei82640-04-8.mol

Raloxifene hydrochloride physikalisch-chemischer Eigenschaften

Schmelzpunkt	250-253°C
storage temp.	2-8°C
Löslichkeit	DMSO: 28 mg/mL, soluble
Aggregatzustand	solid
Farbe	light yellow
maximale Wellenlänge (λmax)	286nm(lit.)
Merck	14,8098
BCS Class	2
InChIKey	BKXVVCILCIUCLG-UHFFFAOYSA-N
SMILES	C1(C(=O)C2C=CC(OCCN3CCCCC3)=CC=2)C2C=CC(O)=CC=2SC=1C1C=CC(O)=CC=1.Cl
CAS Datenbank	82640-04-8(CAS DataBase Reference)

Sicherheit

Kennzeichnung gefährlicher	Xi
R-Sätze:	36/37/38
S-Sätze:	22-24/25
WGK Germany	3
RTECS-Nr.	PC4956925
HS Code	2934990002

Gefahreninformationscode (GHS)

Raloxifene hydrochloride Chemische Eigenschaften,Einsatz,Produktion Methoden

R-Sätze Betriebsanweisung:
R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.
S-Sätze Betriebsanweisung:
S22:Staub nicht einatmen.
S24/25:Berührung mit den Augen und der Haut vermeiden.
Beschreibung
Raloxifene was launched as Evista in the US for the prevention of postmenopausal osteoporosis. It is noteworthy that this molecule was formerly under development as keoxifene for breast cancer and prostatic hypertrophy. Raloxifene can be prepared by acylation of 6-methoxy-2-(4-methoxyphenyl) benzothiophene followed by simultaneous demethylation of both methoxy groups. Raloxifen is a selective estrogen receptor modulator, exerting antiestrogenic action on certain tissues (breast) and also estrogenic action on bone metabolism or serum lipids. In normal early postmenopausal women, 200 mg daily produced a trend towards suppression of estrogen effects. Raloxifen impeded bone loss in osteoporosis. A two-year study in postmenopausal women with an increased risk for osteoporosis showed that Raloxifen markedly prevented non-traumatic vertebral fractures. Results of several clinical studies demonstrated that Raloxifen appreciably reduced the risk of developing breast cancer. Moreover, it had favourable effect on lipid profiles without having the potential side-effects of estrogen-based therapies. Several extensions for different uses of this molecule are planned, for example growth disorder, obesity, colon tumor and skin atrophy. No serious drug-related events have been reported in the limited number of clinical trials.
Chemische Eigenschaften
Light-Yellow Solid
Originator
Lilly (US)
Verwenden
Labeled Raloxifene, intended for use as an internal standard for the quantification of Raloxifene by GC- or LC-mass spectrometry.
Verwenden
amino acid, nutrient. A nonsteroidal, selective estrogen receptor modulator (SERM). Antiosteoporotic.Insoluble in water.
Verwenden
Raloxifene hydrochloride can be used as a nonsteroidal, selective estrogen receptor modulator (SERM). Antiosteoporotic.
Definition
ChEBI: A hydrochloride salt resulting from the reaction of equimolar amounts of raloxifene and hydrogen chloride.
Trademarks
Evista (Lilly).
Allgemeine Beschreibung
Pharmaceutical secondary standards for application in quality control provide pharma laboratories and manufacturers with a convenient and cost-effective alternative to the preparation of in-house working standards
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.
Clinical Use
Treatment and prevention of osteoporosis in post menopausal women
Arzneimittelwechselwirkung
Potentially hazardous interactions with other drugs
Anticoagulants: antagonism of anticoagulant effect of coumarins.
Colestyramine: reduced absorption of raloxifene - avoid.
Stoffwechsel
Raloxifene undergoes extensive first pass metabolism to the glucuronide conjugates: raloxifene-4'- glucuronide, raloxifene-6-glucuronide, and raloxifene-6, 4′-diglucuronide.
Raloxifene undergoes enterohepatic recycling, and is excreted almost entirely in the faeces. Less than 6% of dose is excreted in the urine.
Lager
+4°C (desiccate)
Einzelnachweise
[1] obach rs.potent inhibition of human liver aldehyde oxidase by raloxifene.

Raloxifene hydrochloride Upstream-Materialien And Downstream Produkte

Raloxifene hydrochloride Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

82640-04-8, Raloxifene hydrochloride Verwandte Suche:

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