(R)-Elagolix
CAS No. : 834153-87-6
(Synonyms: NBI-56418)
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|---|---|---|
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| 50mg | $290 | In-stock |
| 100mg | $460 | In-stock |
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| Cat. No. : | HY-14789 |
| M.Wt: | 631.59 |
| Formula: | C32H30F5N3O5 |
| Purity: | >98 % |
| Solubility: | DMSO : 62.5 mg/mL (ultrasonic;warming;heat to 60°C) |
Elagolix is a highly effective, selective, oral-active, short-term, 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. [1][2][3][4][5].
In Vitro: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].
In Vivo:
Main pharmacokinetic parameters after taking a single oral dose of elagolix to rats[3]
| 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 |