Tibolone

한글명:Tibolone

카스 번호5630-53-5

상품명:Tibolone

CBNumberCB9453050

분자식C21H28O2

포뮬러 무게312.45

MOL 파일5630-53-5.mol

화학적 성질

녹는점	169 °C
끓는 점	447.4±45.0 °C(Predicted)
밀도	1.13±0.1 g/cm3(Predicted)
굴절률	105 ° (C=0.54, CH2Cl2/Et2O)
저장 조건	2-8°C
용해도	DMSO: 용해성15mg/mL, 투명
산도 계수 (pKa)	13.10±0.60(Predicted)
색상	흰색에서 베이지색
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 데이터베이스	5630-53-5(CAS DataBase Reference)

위험 및 안전 성명

위험품 표기

위험 카페고리 넘버

51/53

안전지침서

22-24/25-61

유엔번호(UN No.)

UN 3077 9/PG 3

RTECS 번호

RC8964020

NFPA 704:

	0
2		0

그림문자(GHS)

Tibolone MSDS

Tibolone 화학적 특성, 용도, 생산

개요
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.
화학적 성질
White Solid
용도
A synthetic steroid with weak estrogenic, androgenic and progestogenic activity. A pharamceutical used in the treatment of menopausal syndrome
정의
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.
Pharmacokinetics
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.
부작용
The most common reason for patient withdrawal from clinical trials was vaginal bleeding (also a common side effect when estrogen therapy is used).

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