SML4059
Elagolix sodium
≥98% (HPLC)
别名:
(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 sodium salt, Elagolix sodium salt, NBI 56418, NBI-56418, NBI56418
质量水平
方案
≥98% (HPLC)
表单
powder
储存条件
desiccated
颜色
white to beige
溶解性
H2O: 2 mg/mL, clear
储存温度
-10 to -25°C
SMILES字符串
CC1=C(C2=C(C(OC)=CC=C2)F)C(N(C(N1CC3=C(C=CC=C3F)C(F)(F)F)=O)C[C@@H](C4=CC=CC=C4)NCCCC(O[Na])=O)=O
生化/生理作用
Orally active human gonadotropin releasing hormone (GnRH)/luteinizing hormone releasing hormone (LHRH) receptor (GnRHR, LHRHR) antagonist.
Elagolix is an orally active, potent, high-affinity human gonadotropin-releasing hormone (GnRH)/luteinizing hormone-releasing hormone (LH-RH) receptor (GnRHR, LHRHR) antagonist (Ki = 0.9 nM/human, 3.3 nM/monkey, 4.4 µM/rat) that effectively blocks GnRH-induced inositol phosphate production in RBL-1 hGnRH-R transfectants (IC50 = 1.5 nM against 6 nM GnRH). Oral administration in castrated male cynomolgus macaques effectively reduces circulating LH in a reversible manner in vivo (75% reduction 8h post 30 mg/kg p.o.).
Elagolix is an orally active, potent, high-affinity human gonadotropin-releasing hormone (GnRH)/luteinizing hormone-releasing hormone (LH-RH) receptor (GnRHR, LHRHR) antagonist (Ki = 0.9 nM/human, 3.3 nM/monkey, 4.4 µM/rat) that effectively blocks GnRH-induced inositol phosphate production in RBL-1 hGnRH-R transfectants (IC50 = 1.5 nM against 6 nM GnRH). Oral administration in castrated male cynomolgus macaques effectively reduces circulating LH in a reversible manner in vivo (75% reduction 8h post 30 mg/kg p.o.).
免责声明
Hygroscopic
警示用语：
Warning
危险声明
危险分类
Repr. 2
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
此项目有
Cai-Ping Chen et al.
The Journal of international medical research, 50(3), 3000605221082895-3000605221082895 (2022-03-11)
Gonadotropin-releasing hormone receptor (GnRHR) is expressed in several malignant tumors and inhibits the proliferation and metastasis of cancer cells, but its role in triple-negative breast cancers (TNBCs) is unclear. This study investigated the biological effects of GnRHR and their influence
Chen Chen et al.
Journal of medicinal chemistry, 51(23), 7478-7485 (2008-11-14)
The discovery of novel uracil phenylethylamines bearing a butyric acid as potent human gonadotropin-releasing hormone receptor (hGnRH-R) antagonists is described. A major focus of this optimization was to improve the CYP3A4 inhibition liability of these uracils while maintaining their GnRH-R
Danielle Wright et al.
F&S science, 3(3), 299-308 (2022-08-18)
To determine the effect relugolix and elagolix have on the production of extracellular matrix (ECM) proteins in human leiomyoma cells. Laboratory study. University hospital. None. January 5, 2022 Cell culture, protein analysis, immunohistochemistry. Production of GnRHR, COL1A1, FN1, VCAN, p-ERK
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