ラロキシフェン

化学名:ラロキシフェン

CAS番号.84449-90-1

英語名:Raloxifene

CBNumberCB1290431

MFC28H27NO4S

MW473.58

MOL File84449-90-1.mol

别名

[2-(4-ヒドロキシフェニル)-6-ヒドロキシベンゾ[b]チオフェン-3-イル][4-[2-(1-ピペリジニル)エトキシ]フェニル]ケトン

2-(4-ヒドロキシフェニル)-6-ヒドロキシ-1-ベンゾチオフェン-3-イル4-(2-ピペリジノエトキシ)フェニルケトン

ラロキシフェン

ラロキシフェン物理性質

融点	250-253°C
沸点	728.2±60.0 °C(Predicted)
比重(密度)	1.289±0.06 g/cm3(Predicted)
貯蔵温度	Desiccate at +4°C
溶解性	DMSO: 28 mg/mL、可溶
外見	個体
酸解離定数(Pka)	8.83±0.15(Predicted)
色	ライトイエロー
水溶解度	560μg/L at 25℃
LogP	6.09
CAS データベース	84449-90-1(CAS DataBase Reference)

安全性情報

WGK Germany	3
HSコード	29349990
有毒物質データの	84449-90-1(Hazardous Substances Data)

危険有害性情報のコード(GHS)

MSDS Information

ラロキシフェン化学特性,用途語,生産方法

効能
骨粗鬆症治療薬, 選択的エストロゲン受容体モジュレータ (SERM)
化学的特性
Light-Yellow Solid
使用
Raloxifene is a nonsteroidal, selective estrogen receptor modulator (SERM). Antiosteoporotic.
適応症
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.
定義
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member of the class of 1-benzothiophenes that is 1-benzothiophene in which the hydrogens at positions 2, 3, and 6 have been replaced by p-hydroxyphenyl, p-[2-(piperidin-1-yl)ethoxy]benzoyl, and hydroxy groups, respectively.
一般的な説明
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.
生物活性
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.
臨床応用
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.

ラロキシフェン上流と下流の製品情報

ラロキシフェン生産企業

84449-90-1, ラロキシフェンキーワード

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ラロキシフェン

危険有害性情報のコード(GHS)

MSDS Information

ラロキシフェン 化学特性,用途語,生産方法

ラロキシフェン 上流と下流の製品情報

ラロキシフェン 生産企業

84449-90-1, ラロキシフェン キーワード

ラロキシフェン化学特性,用途語,生産方法

ラロキシフェン上流と下流の製品情報

ラロキシフェン生産企業

84449-90-1, ラロキシフェンキーワード