- Shanghai Jizhi Biochemical Technology Co., Ltd
- China
- Product Name: Elagolix sodium
- Price: ￥816.0/100mg ￥1626.0/250mg ￥13386.0/5g ￥4056.0/1g
- Purity: 97.0%
- Stocking Period: 2 Day
- Contact: Liu jia
- DC Chemicals Limited
- China
- Product Name: Elagolix
- Price: $Inquiry/100mg $Inquiry/250mg $Inquiry/500mg
- Purity: 98.0%
- Stocking Period: 3 Day
- Contact: Tony Cao
- Dayang Chem (Hangzhou) Co., Ltd.
- China
- Product Name: NBI 56418NA
- Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
- Purity: 98.0%
- Stocking Period: Inquiry
- Contact: Ms Wang
- Zhejiang Hangyu API Co., Ltd
- China
- Product Name: Elagolix
- Price: ￥Inquiry/1kg
- Purity: 99.5%
- Stocking Period: Inquiry
- Contact: Vinnie
- Henan Tianfu Chemical Co., Ltd.
- China
- Product Name: Evillagoli sodium
- Price: $Inquiry/1kg $Inquiry/25kg $Inquiry/1000kg $Inquiry/10ton
- Purity: 99.0%
- Stocking Period: Inquiry
- Contact: Anson
832720-36-2
832720-36-2 structure
- Name: Elagolix sodium
- Chemical 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
- CAS Number: 832720-36-2
- Molecular Formula: C32H29F5N3NaO5
- Molecular Weight: 653.571
- Catalog: Signaling Pathways GPCR/G Protein GNRH Receptor
- Create Date: 2018-03-17 08:00:00
- Modify Date: 2024-01-02 19:53:09
-
Elagolix 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 |
|---|---|
| Synonyms |
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 |
| 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℃ |