エラゴリクス
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- CAS番号.
- 834153-87-6
- 化学名:
- エラゴリクス
- 别名:
- エラゴリクス;エラゴリックス;4-{[(1R)-2-[5-(2-フルオロ-3-メトキシフェニル)-3-{[2-フルオロ-6-(トリフルオロメチル)フェニル]メチル}-4-メチル-2,6-ジオキソ-1,2,3,6-テトラヒドロピリミジン-1-イル]-1-フェニルエチル]アミノ}ブタン酸;4-[[(1R)-1-フェニル-2-[2,6-ジオキソ-3-[2-フルオロ-6-(トリフルオロメチル)ベンジル]-4-メチル-5-(2-フルオロ-3-メトキシフェニル)-1,2,3,6-テトラヒドロピリミジン-1-イル]エチル]アミノ]酪酸
- 英語名:
- elagolix
- 英語别名:
- Elagoli;NBI 56418;(R)-4-((2-(5-(2-fluoro-3-methoxyphenyl)-3-(2-fluoro-6-(trifluoromethyl)benzyl)-4-methyl-2,6-dioxo-3,6-dihydropyrimidin-1(2H)-yl)-1-phenylethyl)amino)butanoic acid;CS-2232;CS-2011;ABT-620;elagolix;Elagolix-d6;(R)-Elagolix;Elagolix
CAS
- CBNumber:
- CB51518509
- 化学式:
- C32H30F5N3O5
- 分子量:
- 631.59
- MOL File:
- 834153-87-6.mol
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エラゴリクス 物理性質
- 沸点 :
- 728.6±70.0 °C(Predicted)
- 比重(密度) :
- 1.350
- 貯蔵温度 :
- Store at -20°C
- 溶解性:
- DMSO : ≥ 100 mg/mL (158.33 mM)
- 酸解離定数(Pka):
- 4.40±0.10(Predicted)
安全性情報
- リスクと安全性に関する声明
- 危険有害性情報のコード(GHS)
| 絵表示（GHS） |
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| 注意喚起語 |
危険 |
| 危険有害性情報 |
| コード |
危険有害性情報 |
危険有害性クラス |
区分 |
注意喚起語 |
シンボル |
P コード |
| H360 |
生殖能または胎児への悪影響のおそれ |
生殖毒性 |
1A, 1B |
危険 |
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| 注意書き |
| P201 |
使用前に取扱説明書を入手すること。 |
| P202 |
全ての安全注意を読み理解するまで取り扱わないこ と。 |
| P280 |
保護手袋/保護衣/保護眼鏡/保護面を着用するこ と。 |
| P308+P313 |
暴露または暴露の懸念がある場合：医師の診断/手当てを 受けること。 |
| P405 |
施錠して保管すること。 |
| P501 |
内容物/容器を．．．に廃棄すること。 |
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エラゴリクス 価格
| メーカー |
製品番号 |
製品説明 |
CAS番号 |
包装 |
価格 |
更新時間 |
購入 |
エラゴリクス 化学特性,用途語,生産方法
効能
子宮内膜症治療薬, 性腺刺激ホルモン放出ホルモン受容体拮抗薬
説明
Elagolix is a gonadotropin-releasing hormone(GnRH) receptor antagonist indicated for the management of moderate to severe pain associated with endometriosis. Elagolix is an orally administered,nonpeptide small molecule gonadotropin-releasing hormone(GnRH) receptor antagonist that inhibits endogenousGnRH signaling by binding competitively to GnRH receptors in the pituitary gland.
Elagolix results in dose-dependent suppression of luteinizing hormone(LH) and follicle-stimulating hormone(FSH) leading to decreased blood leveis of the ovarian sex hormones, estradiol and progesterone.Elagolix causes a dose-dependent decrease in bone mineral density (BMD).BMD loss is greater with increasing duration of use and may not be completely reversible after stopping treatment.
As milk production is dependent on at least minimal levels of estrogen, this product may reduce milk production.
使用
Elagolix has a potential role for treating uterine bleeding associated to uterine myomas. Elagolix is also used in the methods for treatment of estrogen-dependent disorders including gonadotropin-releasing hormone (GnRH) antagonists in combination with add-back therapy.
製造方法
Elagolix was a gonadotropin-releasing hormone antagonist. It was approved in 2018 by FDA via priority review for clinical treatment of endometriosis. Based on retrosynthetic analysis, five reported synthesis routes of elagolix were summarized. They were compared and evaluated in terms of step numbers, total yields, costs, synthetic conditions and manufacturing safety. At last, the synthetic method of d6-elagolix was introduced. This review would be beneficial to the future process researches of elagolix and its deuterium analogues.
Recent Progress in the Synthesis of ElagolixDiscovery of sodium R-(+)-4-{2-[5-(2-fluoro-3-methoxyphenyl)-3-(2-fluoro-6-[trifluoromethyl]benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenylethylamino}butyrate (elagolix), a potent and orally available nonpeptide antagonist of the human gonadotropin-releasing hormone receptor
エラゴリクス 上流と下流の製品情報
原材料
準備製品
エラゴリクス 生産企業
Global( 190)Suppliers
834153-87-6(エラゴリクス)キーワード:
- 834153-87-6
- elagolix
- 4-[[(1R)-2-[5-(2-Fluoro-3-methoxyphenyl)-3-[[2-fluoro-6-(trifluoromethyl)phenyl]methyl]-3,6-dihydro-4-methyl-2,6-dioxo-1(2H)-pyrimidinyl]-1-phenylethyl]amino]butanoic acid
- Butanoic acid, 4-[[(1R)-2-[5-(2-fluoro-3-methoxyphenyl)-3-[[2-fluoro-6-(trifluoromethyl)phenyl]methyl]-3,6-dihydro-4-methyl-2,6-dioxo-1(2H)-pyrimidinyl]-1-phenylethyl]amino]-
- 4-({(1R)-2-[5-(2-Fluoro-3-methoxyphenyl)-3-[2-fluoro-6-(trifluoromethyl)benzyl]-4-methyl-2,6-dioxo-3,6-dihydro-1(2H)-pyrimidinyl]-1-phenylethyl}amino)butanoic acid
- 4-[[(1R)-2-[5-(2-FLUORO-3-METHOXYPHENYL)-3-[[2-FLUORO-6-(TRIFLUOROMETHYL)PHENYL]METHYL]-4-METHYL-2,6-DIOXOPYRIMIDIN-1-YL]-1-PHENYLETHYL]AMINO]BUTANOIC ACID
- elagolix USP/EP/BP
- Seviram hydrochloride
- Elagolix (NBI-56418)
- CS-2011
- CS-2232
- Elagolix-004-R
- NBI 56418; NBI56418;NBI-56418
- (R)-4-{2-[5-(2-fluoro-3-methoxyphenyl)-3-[2-fluoro-6-(trifluoromethyl)benzyl]-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenylethylamino}butyric acid
- (R)-Elagolix
- ABT-620
- Elagolix-d6
- NBI 56418
- (R)-4-((2-(5-(2-fluoro-3-methoxyphenyl)-3-(2-fluoro-6-(trifluoromethyl)benzyl)-4-methyl-2,6-dioxo-3,6-dihydropyrimidin-1(2H)-yl)-1-phenylethyl)amino)butanoic acid
- Elagoli
- Elagolix Sodium Monomer
- Tropicamide Impurity 35
- Elagolix sodium
4-[[(1R)-2-[5-(2-Fluoro-3-methoxyphenyl)-3-[[2-fluoro-6- (trifluoromethyl)phenyl]methyl]-3,6-dihydro-4-methyl-2,6- dioxo-1(2H)-pyrimidinyl]-1-phenylethyl]amino]butanoic acid
- Elagolix
CAS
- エラゴリクス
- エラゴリックス
- 4-{[(1R)-2-[5-(2-フルオロ-3-メトキシフェニル)-3-{[2-フルオロ-6-(トリフルオロメチル)フェニル]メチル}-4-メチル-2,6-ジオキソ-1,2,3,6-テトラヒドロピリミジン-1-イル]-1-フェニルエチル]アミノ}ブタン酸
- 4-[[(1R)-1-フェニル-2-[2,6-ジオキソ-3-[2-フルオロ-6-(トリフルオロメチル)ベンジル]-4-メチル-5-(2-フルオロ-3-メトキシフェニル)-1,2,3,6-テトラヒドロピリミジン-1-イル]エチル]アミノ]酪酸