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Elagolix is an orally active, highly effective, selective non-peptide antagonist of the gonadotropin-releasing hormone receptor (GnRH receptor) with a dissociation constant (KD) of 54 pM, as well as an NFAT inhibitor, and is utilized in researching endometriosis-related pain.
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
| Description | Elagolix is an orally active, highly effective, selective non-peptide antagonist of the gonadotropin-releasing hormone receptor (GnRH receptor) with a dissociation constant (KD) of 54 pM, as well as an NFAT inhibitor, and is utilized in researching endometriosis-related pain. |
| In vitro | Elagolix is a human GnRH receptor (GnRHR) antagonist with an IC50 of 0.25 nM in kinase assays. It also demonstrates NFAT inhibition with an IC50 of 5.4 nM and effectively blocks Ca2+ flux, with an IC50 of 0.86 nM. Additionally, Elagolix is a GnRH receptor antagonist with a K i value of 3.7 nM. |
| In vivo | After a single oral dose of Elagolix in rats, the primary pharmacokinetic parameters were as follows:Route Dose (mg/kg) AUC 0→t (ng•h/mL) AUC 0→∞ (ng•h/mL) t 1/2 (h) T max (h) C max (ng/mL) Oral 15 5212 5301 6.56 1.50 1515. |
| Molecular Weight | 631.6 |
| Formula | C32H30F5N3O5 |
| Cas No. | 2323071-30-1 |
| Smiles | O=C(O)CCCNC(C=1C=CC=CC1)CN2C(=O)C(C=3C=CC=C(OC)C3F)=C(N(C2=O)CC=4C(F)=CC=CC4C(F)(F)F)C |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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