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Elagolix Sodium

CAS No.
832720-36-2
Chemical Name:
Elagolix Sodium
Synonyms
elagolix sodium salt;NBI 56418NA;4-{2-[5-(2-fluoro-3-methoxy-phenyl)-3-(2-fluoro-6-trifluoromethyl-benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenyl-ethylamino}-butyrate;sodium (R)-4-((2-(5-(2-fluoro-3-methoxyphenyl)-3-(2-fluoro-6-(trifluoromethyl)benzyl)-4-methyl-2,6-dioxo-2,3-dihydropyrimidin-1(6H)-yl)-1-phenylethyl)amino)butanoate;Elagollix;Elagolix sodiu;Elagolix sodiuM;Flagolix Sodium;NBI-56418 sodium;Orilissaelagolix
CBNumber:
CB92627794
Molecular Formula:
C32H29F5N3NaO5
Molecular Weight:
653.571546
MDL Number:
MFCD12546649
MOL File:
832720-36-2.mol
Last updated:2024-04-24 17:21:45

Elagolix Sodium Properties

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
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

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS08
Signal word  Danger
Hazard statements  H304-H361
Precautionary statements  P201-P202-P281-P308+P313-P405-P501

Elagolix Sodium price More Price(13)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 26534 Elagolix (sodium salt) 832720-36-2 5mg $81 2024-03-01 Buy
Cayman Chemical 26534 Elagolix (sodium salt) 832720-36-2 25mg $317 2024-03-01 Buy
Cayman Chemical 26534 Elagolix (sodium salt) 832720-36-2 10mg $143 2024-03-01 Buy
TRC E501018 ElagolixSodium 832720-36-2 100mg $65 2021-12-16 Buy
ChemScene CS-0003317 Elagolixsodium 99.66% 832720-36-2 5mg $70 2021-12-16 Buy
Product number Packaging Price Buy
26534 5mg $81 Buy
26534 25mg $317 Buy
26534 10mg $143 Buy
E501018 100mg $65 Buy
CS-0003317 5mg $70 Buy

Elagolix Sodium Chemical Properties,Uses,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.

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

Global( 262)Suppliers
Supplier Tel Email Country ProdList Advantage
Hebei Mojin Biotechnology Co., Ltd
+8613288715578 sales@hbmojin.com China 12456 58
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010-60279497 sales01@cooperate-pharm.com CHINA 1811 55
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008657128800458; +8615858145714 fandachem@gmail.com China 9348 55
Shanghai Yingrui Biopharma Co., Ltd.
+86-21-33585366 - 03@ sales03@shyrchem.com CHINA 738 60
ATK CHEMICAL COMPANY LIMITED
+undefined-21-51877795 ivan@atkchemical.com China 32480 60
career henan chemical co
+86-0371-86658258 sales@coreychem.com China 29914 58

Related articles

View Lastest Price from Elagolix Sodium manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
Elagolix Sodium pictures 2024-04-24 Elagolix Sodium
832720-36-2
US $50.00 / kg 1kg 99.10% 50000kg Ouhuang Engineering Materials (Hubei) Co., Ltd
Elagolix Sodium pictures 2024-04-07 Elagolix Sodium
832720-36-2
US $100.00 / kg 1kg 99% 1t Zibo Wei Bin Import & Export Trade Co. Ltd.
Elagolix Sodium pictures 2024-03-12 Elagolix Sodium
832720-36-2
US $0.00 / g 1g 98% HPLC 100kg shandong perfect biotechnology co.ltd
  • Elagolix Sodium pictures
  • Elagolix Sodium
    832720-36-2
  • US $50.00 / kg
  • 99.10%
  • Ouhuang Engineering Materials (Hubei) Co., Ltd
  • Elagolix Sodium pictures
  • Elagolix Sodium
    832720-36-2
  • US $100.00 / kg
  • 99%
  • Zibo Wei Bin Import & Export Trade Co. Ltd.
  • Elagolix Sodium pictures
  • Elagolix Sodium
    832720-36-2
  • US $0.00 / g
  • 98% HPLC
  • shandong perfect biotechnology co.ltd
Elagolix sodiuM NBI 56418NA(elagolix na) Elagolix sodiu Elagollix 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 NBI-56418 sodium Evillagoli sodium sodium (R)-4-((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 Orilissaelagolix Flagolix Sodium odium 4-[[(1R)-2-[5-(2-fluoro-3-methoxy-phenyl)-3-[[2-fluoro-6- sodium 4-[[(1R)-2-[5-(2-fluoro-3-methoxy-phenyl)-3-[[2-fluor... 4-{2-[5-(2-fluoro-3-methoxy-phenyl)-3-(2-fluoro-6-trifluoromethyl-benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenyl-ethylamino}-butyrateChemicalbook Elagolix-d6 SodiumQ: What is Elagolix-d6 Sodium Q: What is the CAS Number of Elagolix-d6 Sodium NBI 56418NA 4-{2-[5-(2-fluoro-3-methoxy-phenyl)-3-(2-fluoro-6-trifluoromethyl-benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenyl-ethylamino}-butyrate elagolix sodium salt sodium (R)-4-((2-(5-(2-fluoro-3-methoxyphenyl)-3-(2-fluoro-6-(trifluoromethyl)benzyl)-4-methyl-2,6-dioxo-2,3-dihydropyrimidin-1(6H)-yl)-1-phenylethyl)amino)butanoate Sodium 4-{[(1R)-2-[5-(2-fluoro-3-methoxyphenyl)-3-{[2-fluoro-6-(trifluoromethyl)phenyl]methyl}-4-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-1-yl]-1-phenylethyl]amino}butanoate 832720-36-2 C32H29F5N3O5Na C32H29F5N3NaO5 API