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Элаголикс
- английское имяelagolix
- CAS №834153-87-6
- CBNumberCB51518509
- ФормулаC32H30F5N3O5
- мольный вес631.59
- номер MDLMFCD11973645
- файл Mol834153-87-6.mol
химическое свойство
Температура кипения | 728.6±70.0 °C(Predicted) |
плотность | 1.350 |
температура хранения | Store at -20°C |
растворимость | DMSO : ≥ 100 mg/mL (158.33 mM) |
пка | 4.40±0.10(Predicted) |
форма | Solid |
цвет | White to off-white |
ИнЧИКей | HEAUOKZIVMZVQL-VWLOTQADSA-N |
SMILES | C(O)(=O)CCCN[C@H](C1=CC=CC=C1)CN1C(=O)N(CC2=C(C(F)(F)F)C=CC=C2F)C(C)=C(C2=CC=CC(OC)=C2F)C1=O |
FDA UNII | 5B2546MB5Z |
Словарь наркотиков NCI | elagolix |
Код УВД | H01CC03 |
рисовальное письмо(GHS)
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рисовальное письмо(GHS)
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сигнальный язык
опасность
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вредная бумага
H360:Может отрицательно повлиять на способность к деторождению или на неродившегося ребенка.
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оператор предупредительных мер
P201:Беречь от тепла, горячих поверхностей, искр, открытого огня и других источников воспламенения. Не курить.
P202:Перед использованием ознакомиться с инструкциями по технике безопасности.
P280:Использовать перчатки/ средства защиты глаз/ лица.
P308+P313:ПРИ подозрении на возможность воздействия обратиться за медицинской помощью.
P405:Хранить в недоступном для посторонних месте.
P501:Удалить содержимое/ контейнер на утвержденных станциях утилизации отходов.
Элаголикс химические свойства, назначение, производство
Описание
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.
Использование
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.Подготовка
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 Elagolix
Discovery 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
Элаголикс запасные части и сырье
сырьё
- 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]-, ethyl ester
- 3-[(2R)-2-Amino-2-phenylethyl]-5-(2-fluoro-3-methoxyphenyl)-1-[[2-fluoro-6-(trifluoromethyl)phenyl]methyl]-6-methyl-2,4(1H,3H)-pyrimidinedione
- Метил-4-бромбутира
Элаголикс поставщик
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