SML4059
Elagolix sodium
≥98% (HPLC)
别名:
NBI56418, (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
SMILES string
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
assay
≥98% (HPLC)
form
powder
storage condition
desiccated
color
white to beige
solubility
H2O: 2 mg/mL, clear
storage temp.
-10 to -25°C
Quality Level
Biochem/physiol Actions
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.).
Disclaimer
Hygroscopic
signalword
Warning
hcodes
Hazard Classifications
Repr. 2
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_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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