GLPBio

Elagolix

Catalog No.: GC19135Purity:>98.00%
COASDSData Sheet
Elagolix ist ein hochpotenter, selektiver, oral wirksamer, nicht peptidischer Antagonist mit kurzer Wirkungsdauer des Gonadotropin-Releasing-Hormon-Rezeptors (GnRHR) (KD = 54 pM).

Die Produkte sind ausschließlich für Forschungszwecke bestimmt. Nicht zur Anwendung am Menschen. Wir verkaufen nicht an Patienten.

Elagolix
Cas No.: 834153-87-6
10mM (in 1mL DMSO)In Stock
$60.00
1
5mgIn Stock
$42.00
1
10mgIn Stock
$63.00
1
25mgIn Stock
$126.00
1
50mgIn Stock
$203.00
1
100mgIn Stock
$322.00
1
Tel: (909) 407-4943 / (909) 689-7124Email: sales@glpbio.com

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    632, 686–694 (2024)
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    Nature
    618, 1017–1023 (2023)
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    Nature
    610, 366–372 (2022)
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    Cell
    187(9):2288-2304 (2024)
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    Cell
    183(7):1867-1883 (2020)
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    Science
    388(6745) (2025)
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    35, 97–116 (2025)
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    33, 273–287 (2023)
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    33, 546–561 (2023)
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    33, 904–922 (2023)
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    31, 1291–1307 (2021)

Beschreibung (Description)

Elagolix is a highly potent, selective, orally-active, short-duration, non-peptide antagonist of the gonadotropin-releasing hormone receptor (GnRHR) (IC50=0.94nM) [1]. Elagolix inhibits the secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) by blocking the endogenous GnRH signaling pathway, thereby reducing the production of estradiol and progesterone[2]. Elagolix has been widely used in various studies to alleviate endometriosis and improve uterine fibroids[3].

In vitro, Elagolix treatment at 100μM for 1h inhibited inositol-1-phosphate accumulation induced by GnRH peptide in HEK293T cells[4]. Treatment with 100nM Elagolix for 48 hours significantly reduced the expression level of COL1A1 and inhibited the MAPK pathway in leiomyoma cells [5].

In vivo, Elagolix treatment via oral administration at a dose of 30mg/kg for 4h reduced the LH levels in castrated male cynomolgus macaques[6].

References:
[1] Kim S M, Lee M, Lee S Y, et al. Discovery of an orally bioavailable gonadotropin-releasing hormone receptor antagonist[J]. Journal of Medicinal Chemistry, 2016, 59(19): 9150-9172.
[2] Lamb Y N. Elagolix: first global approval[J]. Drugs, 2018, 78(14): 1501-1508.
[3] Ciceri S, Colombo D, Fassi E M A, et al. Elagolix Sodium Salt and Its Synthetic Intermediates: A Spectroscopic, Crystallographic, and Conformational Study[J]. Molecules, 2023, 28(9): 3861.
[4] Ciceri S, Fassi E M A, Vezzoli V, et al. Novel non-peptide uracil-derived human gonadotropin-releasing hormone receptor antagonists[J]. European Journal of Medicinal Chemistry, 2024, 279: 116903.
[5] Wright D, Britten J, Malik M, et al. Relugolix and elagolix directly inhibit leiomyoma extracellular matrix production in 2-dimesnional and 3-dimensional cell cultures[J]. F&S Science, 2022, 3(3): 299-308.
[6] Chen C, Wu D, Guo Z, et al. 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-2 H-pyrimidin-1-yl]-1-phenylethylamino} butyrate (Elagolix), a Potent and Orally Available Nonpeptide Antagonist of the Human Gonadotropin-Releasing Hormone Receptor[J]. Journal of medicinal chemistry, 2008, 51(23): 7478-7485.

Protokoll (Protocol)

Cell experiment [1]:

Cell lines

HEK293T cells

Preparation Method

The cDNA of the wild-type GnRH1R was subcloned into the pcDNA3.1(+) expression vector with the HA signal, and expressed in HEK293T cells. HEK293T cells were seeded in six-well plates at a density of 3×105 cells per well, and the culture medium was Dulbecco modified Eagle medium supplemented with 10% fetal bovine serum. The cells were pre-treated with Elagolix (100μM) for 1 hour, and then stimulated with the GnRH peptides for 1 hour. The optical density values (OD) were read at 450nm.

Reaction Conditions

100μM; 1h

Applications

Elagolix treatment inhibited inositol-1-phosphate accumulation induced by GnRH peptide in HEK293T cells.
Animal experiment [2]:

Animal models

Male cynomolgus macaques

Preparation Method

A total of six male cynomolgus macaques, aged approximately 3.7-6.5 years, underwent complete testicular resection. Drug administration was carried out at least 4 weeks after the surgery. No sedation was administered to the macaques during the administration, but macaques were temporarily confined outside the cage. A single oral administration of 30mg/kg dose of Elagolix was given, blood samples were collected before and 4 hours after administration to determine the concentration of bioactive LH in the serum samples.

Dosage form

30mg/kg for once; p.o.

Applications

Elagolix treatment reduced the LH levels in castrated male cynomolgus macaques.

References:
[1] Ciceri S, Fassi E M A, Vezzoli V, et al. Novel non-peptide uracil-derived human gonadotropin-releasing hormone receptor antagonists[J]. European Journal of Medicinal Chemistry, 2024, 279: 116903.
[2] Chen C, Wu D, Guo Z, et al. 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-2 H-pyrimidin-1-yl]-1-phenylethylamino} butyrate (Elagolix), a Potent and Orally Available Nonpeptide Antagonist of the Human Gonadotropin-Releasing Hormone Receptor[J]. Journal of medicinal chemistry, 2008, 51(23): 7478-7485.

Produktdokumente (Product Documents)

Purity:>98.00%Appearance:A solid
COASDSData Sheet

Chemische Eigenschaften (Chemical Properties)

CAS-Nr.
834153-87-6
Chemischer Name
(R)-4-((2-(5-(2-fluoro-3-methoxyphenyl)-3-(2-fluoro-6-(trifluoromethyl)benzyl)-4-methyl-2,6-dioxo-2,3-dihydropyrimidin-1(6H)-yl)-1-phenylethyl)amino)butanoic acid
SMILES
O=C(CCCN[C@@H](CN(C1=O)C(N(C(C)=C1C2=CC=CC(OC)=C2F)CC3=C(C=CC=C3F)C(F)(F)F)=O)C4=CC=CC=C4)O
Summenformel
C32H30F5N3O5
Molekulargewicht
631.59
Löslichkeit
DMSO : ≥ 100 mg/mL (158.33 mM)
Lagerung
Store at -20°C
Allgemeine Hinweise
Wählen Sie anhand der Löslichkeitsdaten des Produkts ein geeignetes Lösungsmittel. Aliquotieren Sie die Stammlösung nach der Herstellung, um wiederholte Gefrier-Auftau-Zyklen zu vermeiden.
Verwenden Sie Stammlösungen bei Lagerung bei -80°C innerhalb von 6 Monaten bzw. bei -20°C innerhalb von 1 Monat.
Zur Verbesserung der Löslichkeit das Röhrchen auf 37°C erwärmen und für eine angemessene Dauer beschallen.
Versandbedingungen
Evaluierungsmuster werden mit Kühlakkus versandt. Andere verfügbare Größen werden bei Raumtemperatur oder auf Anfrage mit Kühlakkus versandt.

Rechner (Calculators)Molarität / Verdünnung / Molekulargewicht / Einheitenumrechnung / In-vivo-Formulierung / Löslichkeit

g/mol

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