Raloxifene

한글명:Raloxifene

카스 번호84449-90-1

상품명:Raloxifene

CBNumberCB1290431

분자식C28H27NO4S

포뮬러 무게473.58

MOL 파일84449-90-1.mol

화학적 성질

녹는점	250-253°C
끓는 점	728.2±60.0 °C(Predicted)
밀도	1.289±0.06 g/cm3(Predicted)
저장 조건	Desiccate at +4°C
용해도	DMSO: 28mg/mL, 용해성
물리적 상태	고체
물리적 상태	단단한 모양
산도 계수 (pKa)	8.83±0.15(Predicted)
색상	연노랑
수용성	560μg/L at 25℃
LogP	6.09
CAS 데이터베이스	84449-90-1(CAS DataBase Reference)

위험 및 안전 성명

WGK 독일	3
HS 번호	29349990
유해 물질 데이터	84449-90-1(Hazardous Substances Data)

그림문자(GHS)

Raloxifene MSDS

Raloxifene 화학적 특성, 용도, 생산

화학적 성질
Light-Yellow Solid
용도
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.
정의
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member of the class of 1-benzothiophenes that is 1-benzothiophene in which the hydrogens at positions 2, 3, and 6 have been replaced by p-hydroxyphenyl, p-[2-(piperidin-1-yl)ethoxy]benzoyl, and hydroxy groups, respectively.
일반 설명
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.
생물학적 활성
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.

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