Elagolix sodium
Modify Date: 2024-01-02 19:53:09
Elagolix sodium structure
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Common Name | Elagolix sodium | ||
|---|---|---|---|---|
| CAS Number | 832720-36-2 | Molecular Weight | 653.571 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C32H29F5N3NaO5 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of Elagolix sodiumElagolix sodium is a human GnRH receptor (GnRHR) antagonist with an IC50 and Ki of 0.25 and 3.7 nM, respectively. |
| 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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| Synonym | More Synonyms |
| Description | Elagolix sodium is a human GnRH receptor (GnRHR) antagonist with an IC50 and Ki of 0.25 and 3.7 nM, respectively. |
|---|---|
| Related Catalog | |
| Target |
IC50: 0.25 nM (GnRHR)[1] Ki: 3.7 nM (GnRHR)[2] |
| In Vitro | Elagolix sodium is a human GnRH receptor (GnRHR) antagonist with an IC50 of 0.25 nM in Kinase assay. Elagolix sodium has advanced to phase 3 trials for the treatment of endometriosis and uterine fibroids. Elagolix sodium also shows NFAT inhibition with an IC50 of 5.4 nM and effectively blocks Ca2+ flux with an IC50 of 0.86 nM[1]. Kinase assay also demonstrates that Elagolix sodium is a human GnRH receptor (GnRHR) antagonist with a Ki value of 3.7 nM[2]. |
| Kinase Assay | The affinity of Elagolix sodium for hGnRH-R is determined by a competitive displacement of the radioligand GnRH from membranes prepared from HEK293 cells stably transfected with the full-length human GnRH receptor[2]. |
| Cell Assay | RBL-1 cells stably expressing the human cloned GnRH receptor are seeded into 96 well plates at a density of 15 000 cells per well in inositol-free DMEM containing 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 and are labeled for 48 h with 0.2 μCi myo-2-[3H]inositol. The cells are washed once in PBS and pretreated with assay buffer for 15 to 60 min at 37°C. The cells are then stimulated with GnRH (6 nM) in the presence or absence of Elagolix sodium and incubated for 60 min at 37°C[2]. |
| References |
| Molecular Formula | C32H29F5N3NaO5 |
|---|---|
| Molecular Weight | 653.571 |
| Exact Mass | 653.192505 |
| PSA | 105.39000 |
| LogP | 4.59120 |
| Storage condition | -20℃ |
| Sodium 4-({(1R)-2-[5-(2-fluoro-3-methoxyphenyl)-3-[2-fluoro-6-(trifluoromethyl)benzyl]-4-methyl-2,6-dioxo-3,6-dihydropyrimidin-1(2H)-yl]-1-phenylethyl}amino)butanoate |
| UNII-5948VUI423 |
| Elagolix sodium |
| Butanoic acid, 4-[[(1R)-2-[5-(2-fluoro-3-methoxyphenyl)-3-[[2-fluoro-6-(trifluoromethyl)phenyl]methyl]-3,6-dihydro-4-methyl-2,6-dioxo-1(2H)-pyrimidinyl]-1-phenylethyl]amino]-, sodium salt (1:1) |
| Sodium 4-({(1R)-2-[5-(2-fluoro-3-methoxyphenyl)-3-[2-fluoro-6-(trifluoromethyl)benzyl]-4-methyl-2,6-dioxo-3,6-dihydro-1(2H)-pyrimidinyl]-1-phenylethyl}amino)butanoate |
| Elagolix |
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- China
- Product Name: Evillagoli sodium
- Price: $Inquiry/1kg $Inquiry/25kg $Inquiry/1000kg $Inquiry/10ton
- Purity: 99.0%
- Stocking Period: Inquiry
- Contact: Anson
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