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Elagolix Sodium

Elagolix Sodium Structure
Elagolix Sodium
  • CAS No.832720-36-2
  • Chemical Name:Elagolix Sodium
  • CBNumber:CB92627794
  • Molecular Formula:C32H29F5N3NaO5
  • Formula Weight:653.571546
  • MOL File:832720-36-2.mol
Elagolix Sodium Property
  • Melting point >188°C (dec.)
  • storage temp. Hygroscopic, -20°C Freezer, Under inert atmosphere
  • solubility DMSO (Slightly), Methanol (Slightly)
  • form Solid
  • color White to Off-White
  • Water Solubility H2O: 2mg/mL, clear
  • Stability Hygroscopic
  • InChIKey DQYGXRQUFSRDCH-YEZAQYPZNA-M
  • SMILES [Na+].C([O-])(=O)CCCN[C@H](C1=CC=CC=C1)CN1C(=O)N(CC2=C(C(F)(F)F)C=CC=C2F)C(C)=C(C2=CC=CC(OC)=C2F)C1=O |&1:8,r|
  • FDA UNII 5948VUI423
  • UNSPSC Code 12352200
Hazard and Precautionary Statements (GHS)
  • Symbol(GHS)
  • Signal wordDanger
  • Hazard statements H304-H361
  • Precautionary statements P201-P202-P281-P308+P313-P405-P501

Elagolix Sodium Chemical Properties,Usage,Production

  • Description Elagolix sodium (ABT-620) is a small molecule, orally active gonadotropin-releasing hormone (GnRH) receptor antagonist. It has the ability to suppress estradiol (E2) concentrations in a dose-dependent manner.
    It was originally developed by Neurocrine Biosciences, then licensed to Abbott (now Abbvie) for worldwide co-development of this indication in 2010. AbbVie is applying to use elagolix for the treatment of endometriosis with associated pain. Elagolix is the first orally available GnRH antagonist, and as such may provide patients with relief from the painful symptoms of endometriosis while offering advantages over currently available injectable peptide-based treatments. The estimated patient population is over 170 million women worldwide.
  • Description Elagolix is an antagonist of the gonadotropin-releasing hormone receptor (GnRHR; Ki = 0.9 nM in a radioligand binding assay). It is selective for GnRHR over the cytochrome P450 (CYP) isoform CYP3A4 (IC50 = 56 μM) as well as a panel of 100 receptors, ion channels, enzymes, and transporters (IC50s = >10 μM). Elagolix inhibits GnRH-induced inositol phosphate production in RBL-1 cells expressing human GnRHR (IC50 = 1.5 nM). In vivo, elagolix (30 mg/kg) suppresses production of luteinizing hormone in castrated male cynomolgus macaques. Formulations containing elagolix have been used in the treatment of endometriosis.
  • Chemical Properties Elagolix sodium is a small synthetic molecule chemically known as Sodium 4-({(1R)-2- [5-(2-fluoro-3-methoxyphenyl)-3-{[2-fluoro-6-(trifluoromethyl) phenyl]methyl}-4- methyl -2,6-dioxo-3,6-dihydropyrimidin-1(2H)-yl]-1-phenylethyl} amino)butanoate. The structure was confirmed by mass spectrometry, infrared spectroscopy, nuclear magnetic resonance.
    Elagolix sodium is isolated as a hygroscopic, amorphous white to off-white to light yellow powder.
  • Uses Elagolix Sodium is a gonadotropin releasing hormone antagonist (GnRH antagonist) used in the treatment of pain associated with endometriosis in women. It is also in phase III clinical trials for the treatment of uterine fibroids in women. Endometriosis is a frequent cause of infertility, connected with a chronic pelvic and pre-menstrual pain.
    Elagolix sodium for the treatment of women with moderate to severe endometriosis-associated pain
  • Uses Elagolix Sodium is a novel uracil phenylethylamine that acts as potent human gonadotropin-?releasing hormone receptor (hGnRH-?R) antagonist.
  • Synthesis Reference(s) PROCESS FOR THE PREPARATION OF ELAGOLIX SODIUM AND ITS POLYMORPH
    The US patent number 7056927 B2 discloses, elagolix sodium salt as a white solid and process for its preparation in Example-1; Step-IH.
    synthesis of elagolix sodium
    The US patent number 8765948 B2 discloses a process for preparation of amorphous elagolix sodium by spray drying method and solid dispersion of amorphous elagolix sodium with a polymer.
  • Clinical Use ORILISSA is indicated for the management of moderate to severe pain associated with endometriosis. ORILISSA 150 mg tablets are light pink, oblong, film-coated tablets with “EL 150” debossed on one side. Each tablet contains 155.2 mg of elagolix sodium (equivalent to 150 mg of elagolix) as the active ingredient and the following inactive ingredients: mannitol, sodium carbonate monohydrate, pregelatinized starch, povidone, magnesium stearate, polyvinyl alcohol, titanium dioxide, polyethylene glycol, talc, and carmine high tint.
    Elagolix Sodium
  • 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].
Elagolix Sodium Preparation Products And Raw materials
Raw materials
Preparation Products
Elagolix Sodium Suppliers
Global(293)Suppliers
  • Supplier：
    Capot Chemical Co.,Ltd.
  • Tel：+86-（0）57185586718<br/>+86-13336195806
  • Email：sales@capot.com
  • Country：China
  • ProdList：29730
  • Advantage：60
  • Supplier：
    Henan Tianfu Chemical Co.,Ltd.
  • Tel：+86-0371-55170693<br/>+86-19937530512
  • Email：info@tianfuchem.com
  • Country：China
  • ProdList：21628
  • Advantage：55
  • Supplier：
    career henan chemical co
  • Tel：+86-0371-86658258<br/>+8613203830695
  • Email：sales@coreychem.com
  • Country：China
  • ProdList：29858
  • Advantage：58

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