Elagolix |
Catalog No.GC19135
One-Click Copy Product Info
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Elagolix is a highly potent, selective, orally-active, short-duration, non-peptide antagonist of the gonadotropin-releasing hormone receptor (GnRHR) (KD = 54 pM).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 834153-87-6
Sample solution is provided at 25 µL, 10mM.
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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.
| 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: | |
| Cas No. | 834153-87-6 | SDF | |
| Chemical 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 | ||
| Canonical 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 | ||
| Formula | C32H30F5N3O5 | M.Wt | 631.59 |
| Solubility | DMSO : ≥ 100 mg/mL (158.33 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.5833 mL | 7.9165 mL | 15.8331 mL |
| 5 mM | 316.7 μL | 1.5833 mL | 3.1666 mL |
| 10 mM | 158.3 μL | 791.7 μL | 1.5833 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 19 reference(s) in Google Scholar.)