| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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Purity: ≥98%
Elagolix sodium (NBI56418; ABT-620; Orilissa), the sodium salt of Elagolix, is an orally bioavailable and small molecule antagonist of the gonadotropin-releasing hormone receptor (GnRHR) (KD = 54 pM) approved on 7/23/2018 by FDA for the management of moderate to severe pain associated with endometriosis. Elagolix is a short-acting GnRH antagonist that suppresses ovarian estrogen production in a dose-dependent manner, meaning that higher doses result in full suppression while lower doses only cause partial suppression. Elagolix's non-peptide structure and oral bioavailability make it the leader of a new class of GnRH inhibitors known as second-generation inhibitors.
| Targets |
GnRHR ( IC50 = 0.25 nM ); GnRHR ( Ki = 3.7 nM )
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
The competitive displacement of the radioligand GnRH from membranes prepared from HEK293 cells stably transfected with the full-length human GnRH receptor determines Elagolix sodium's affinity for hGnRH-R.
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| Cell Assay |
The human cloned GnRH receptor-expressing RBL-1 cells are seeded into 96-well plates at a density of 15,000 cells per well using inositol-free DMEM that contains 10% dialyzed FBS, 10 mM HEPES, 2 mM L-glutamine, 1 mM sodium pyruvate, 0.1 mM nonessential amino acids, and 50 μg/mL penicillin/streptomycin. The cells are labeled with 0.2 μCi myo-2-[3H]inositol for 48 hours. The assay buffer (140 mM NaCl, 4 mM KCl, 20 mM HEPES, 8.3 mM glucose, 1 mM MgCl2, 1 mM CaCl2, 10 mM LiCl, and 0.1% BSA) is applied to the cells for 15–60 minutes at 37 °C after they have been initially cleaned in PBS. Following GnRH (6 nM) stimulation, the cells are either left without an antagonist or exposed to it for 60 minutes at 37°C. After extracting the cells using 10 mM formic acid at 4°C for 30 minutes, the lysate is put onto Millipore plates that have 20 μg of Dowex AG1-X8 resin on them. Inositol phosphates are eluted with 1 M ammonium formate/0.1 M formic acid after the plate has been cleaned once in H2O and once in 60 mM ammonium formate/5 mM sodium tetraborate. A Lumaplate is used to transfer the eluate, and a TopCount NXT is used to count it.
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| Animal Protocol |
Rhesus Monkey
10 and 50 mg/kg (oral); 3 and 10 mg/kg (i.v.) p.o. or i.v. |
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| References |
| Molecular Formula |
C32H29F5N3NAO5
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| Molecular Weight |
653.57
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| Exact Mass |
653.19
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| Elemental Analysis |
C, 60.85; H, 4.79; F, 15.04; N, 6.65; O, 12.67
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| CAS # |
832720-36-2
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| Related CAS # |
(R)-Elagolix; 834153-87-6; Elagolix-13C,d3 sodium
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| Appearance |
Solid powder
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| SMILES |
CC1=C(C(=O)N(C(=O)N1CC2=C(C=CC=C2F)C(F)(F)F)C[C@@H](C3=CC=CC=C3)NCCCC(=O)[O-])C4=C(C(=CC=C4)OC)F.[Na+]
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| InChi Key |
DQYGXRQUFSRDCH-UQIIZPHYSA-M
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| InChi Code |
InChI=1S/C32H30F5N3O5.Na/c1-19-28(21-11-6-14-26(45-2)29(21)34)30(43)40(18-25(20-9-4-3-5-10-20)38-16-8-15-27(41)42)31(44)39(19)17-22-23(32(35,36)37)12-7-13-24(22)33;/h3-7,9-14,25,38H,8,15-18H2,1-2H3,(H,41,42);/q;+1/p-1/t25-;/m0./s1
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| Chemical Name |
sodium;4-[[(1R)-2-[5-(2-fluoro-3-methoxyphenyl)-3-[[2-fluoro-6-(trifluoromethyl)phenyl]methyl]-4-methyl-2,6-dioxopyrimidin-1-yl]-1-phenylethyl]amino]butanoate
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.83 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (3.83 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (3.83 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 50 mg/mL (76.50 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5301 mL | 7.6503 mL | 15.3006 mL | |
| 5 mM | 0.3060 mL | 1.5301 mL | 3.0601 mL | |
| 10 mM | 0.1530 mL | 0.7650 mL | 1.5301 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03271489 | Active Recruiting |
Other: Elagolix Placebo Drug: Elagolix |
Heavy Menstrual Bleeding Uterine Fibroids |
AbbVie | September 13, 2017 | Phase 3 |
| NCT04333576 | Recruiting | Drug: Elagolix Drug: Placebo |
Endometriosis | AbbVie | August 10, 2020 | Phase 3 |
| NCT04464187 | Recruiting | N/A | Endometriosis Uterine Fibrioids |
AbbVie | January 6, 2022 | N/A |
| NCT04630990 | Active Recruiting |
N/A | Endometriosis | AbbVie | December 14, 2020 | N/A |
| NCT01620528 | Completed | Drug: elagolix Drug: placebo |
Endometriosis | AbbVie (prior sponsor, Abbott) | May 22, 2012 | Phase 3 |
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