Tibolon

Bezeichnung:Tibolon

CAS-Nr5630-53-5

Englisch Name:Tibolone

CBNumberCB9453050

SummenformelC21H28O2

Molgewicht312.45

MOL-Datei5630-53-5.mol

Synonyma

Tibolon

Tibolon physikalisch-chemischer Eigenschaften

Schmelzpunkt	169 °C
Siedepunkt	447.4±45.0 °C(Predicted)
Dichte	1.13±0.1 g/cm3(Predicted)
Brechungsindex	105 ° (C=0.54, CH2Cl2/Et2O)
storage temp.	2-8°C
Löslichkeit	DMSO: soluble15mg/mL, clear
pka	13.10±0.60(Predicted)
Farbe	white to beige
Merck	9427
InChI	InChI=1/C21H28O2/c1-4-21(23)10-8-18-19-13(2)11-14-12-15(22)5-6-16(14)17(19)7-9-20(18,21)3/h1,13,17-19,23H,5-12H2,2-3H3/t13-,17-,18+,19-,20+,21+/s3
InChIKey	WZDGZWOAQTVYBX-PGFZCDQENA-N
SMILES	[C@@]12([H])[C@H](C)CC3CC(=O)CCC=3[C@@]1([H])CC[C@]1(C)[C@](CC[C@@]21[H])(O)C#C \|&1:0,2,12,16,18,21,r\|
CAS Datenbank	5630-53-5(CAS DataBase Reference)

Sicherheit

Kennzeichnung gefährlicher	N
R-Sätze:	51/53
S-Sätze:	22-24/25-61
RIDADR	UN 3077 9/PG 3
RTECS-Nr.	RC8964020

Gefahreninformationscode (GHS)

Tibolone Chemische Eigenschaften,Einsatz,Produktion Methoden

R-Sätze Betriebsanweisung:
R51/53:Giftig für Wasserorganismen, kann in Gewässern längerfristig schädliche Wirkungen haben.
S-Sätze Betriebsanweisung:
S22:Staub nicht einatmen.
S24/25:Berührung mit den Augen und der Haut vermeiden.
S61:Freisetzung in die Umwelt vermeiden. Besondere Anweisungen einholen/Sicherheitsdatenblatt zu Rate ziehen.
Beschreibung
Tibolone is a synthetic steroid with weak progestational and estrogenic properties, reportedly useful in controlling symptoms resulting from natural or surgical menopause. It has thus far shown no significant antithrombotic effect in post-menopausal patients.
Chemische Eigenschaften
White Solid
Originator
Akzo (Organon) (The Netherklands)
Verwenden
A synthetic steroid with weak estrogenic, androgenic and progestogenic activity. A pharamceutical used in the treatment of menopausal syndrome
Definition
ChEBI: Estran-3-one with a double bond between positions 5 and 10, and bearing both an ethynyl group and a hydroxy group at position 17 (R-configuration). A synthetic steroid hormone drug which acts as an agonist at all five type I steroid hormon receptors, it is used in the prevention of postmenopausal osteoporosis and for treatment of endometriosis.
Trademarks
Livial
Pharmakokinetik
Raloxifene is rapidly absorbed following oral administration, with an estimated 60% absorption, but it has a very low bioavailability (2%), associated with extensive phase II metabolism. The metabolites are excreted via the bile, with potential enterohepatic recycling that could account for the interaction with cholestyramine. Supportive of the enterohepatic recycling is the half-life of 28 hours. Metabolism of raloxifene occurs to a great extent in the intestine and consists of glucuronide conjugation catalyzed by uridine diphosphate glucuronosyltransferase (UGT).
Clinical Use
Tibolone is a synthetic steroid that has been shown to increase bone mineral density similar to alendronate. The U.S. FDA approval is pending; overseas, this agent is used for the treatment of menopausal symptoms as well as the prevention of osteoporosis. It is considered to be a viable alternative to conjugated equine estrogen plus micronized progesterone.
Nebenwirkungen
The most common reason for patient withdrawal from clinical trials was vaginal bleeding (also a common side effect when estrogen therapy is used).

Tibolon Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

5630-53-5, Tibolone Verwandte Suche:

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