Elagolix
Elagolix is an orally active, highly effective, selective and non-peptide gonadotropin-releasing hormone receptor (GnRH receptor) antagonist (KD = 54 pM) and NFAT inhibitor, which can be used to study pain related to endometriosis.
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- CAS. Nr.: 2323071-30-1
- Formel: C32H30F5N3O5
- Molecular Weight:631.59
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Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Biologische Aktivität
Elagolix is a human GnRH receptor (GnRHR) antagonist, with an IC50 of 0.25 nM in kinase assays[1].
Elagolix also shows NFAT inhibitory effects, with an IC50 of 5.4 nM, and effectively blocks Ca2+ flux, with an IC50 of 0.86 nM[1].
Elagolix is a human GnRH receptor (GnRHR) antagonist, with a Ki value of 3.7 nM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Main pharmacokinetic parameters after taking a single oral dose of Elagolix to rats[2]
| Route | Dose (mg/kg) | AUC0→t (ng•h/mL) | AUC0→∞ (ng•h/mL) | t1/2 (h) | Tmax (h) | Cmax (ng/mL) |
| Oral | 15 | 5212 | 5301 | 6.56 | 1.50 | 1515 |