2. GPCR/G Protein Immunology/Inflammation
  3. GnRH Receptor Nuclear Factor of activated T Cells (NFAT)
  4. 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.

For research use only. We do not sell to patients.

Elagolix

Elagolix Chemical Structure

CAS No. : 2323071-30-1

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Elagolix Related Antibodies

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Description

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[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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Elagolix Related Antibodies
In Vivo


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

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

631.59

Formula

C32H30F5N3O5
CAS No.
SMILES

O=C(O)CCCNC(C1=CC=CC=C1)CN(C(N(CC2=C(C(F)(F)F)C=CC=C2F)C(C)=C3C4=CC=CC(OC)=C4F)=O)C3=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Elagolix Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Elagolix2323071-30-1GnRH ReceptorNuclear Factor of activated T Cells (NFAT)Gonadotropin releasing hormone receptorGNRHRGnRHFSHLHuterine fibroidsInhibitorinhibitorinhibit

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