Elagolix sodium | NBI-56418 | CAS#834153-87-6 | | (GnRH) Antagonist

Elagolix sodium
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 201200

CAS#: 832720-36-2 (sodium)

Description: Elagolix, also known as NBI56418 and ABT-620, is a Gonadotropin-Releasing Hormone (GnRH) Antagonist. Elagolix inhibits gonadatropin releasing hormone (GnRH) receptors in the pituitary gland and ultimately reduces circulating sex hormone levels. Elagolix is believed to have its effect by altering the level of pituitary GnRH suppression and, as a result, titrating circulating estrogen levels. Elagolix was approved in 2018.

Chemical Structure

Elagolix sodium

CAS# 832720-36-2 (sodium)

Instruction

Theoretical Analysis

MedKoo Cat#: 201200
Name: Elagolix sodium
CAS#: 832720-36-2 (sodium)
Chemical Formula: C32H29F5N3NaO5
Exact Mass: 0.00
Molecular Weight: 653.570
Elemental Analysis: C, 60.85; H, 4.79; F, 15.04; N, 6.65; O, 12.67

Price and Availability

Size	Price	Availability
100mg	USD 250	2 weeks
200mg	USD 450	2 weeks
500mg	USD 750	2 weeks
1g	USD 1250	2 weeks
2g	USD 1950	2 weeks
5g	USD 3650	2 weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Related CAS #: 834153-87-6 (free acid) 832720-36-2 (sodium)

Synonym: NBI56418 Na; NBI-56418; NBI 56418; ABT-620; ABT 620; ABT620; Elagolix sodium; Orilissa;

IUPAC/Chemical Name: 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

InChi Key: FLFGNMFWNBOBGE-FNNZEKJRSA-N

InChi Code: InChI=1S/C27H45N3O6/c1-2-3-4-5-6-7-8-9-10-11-12-13-14-15-16-17-23(31)35-20-21-24(32)25(33)26(36-21)30-19-18-22(28)29-27(30)34/h9-10,18-19,21,24-26,32-33H,2-8,11-17,20H2,1H3,(H2,28,29,34)/b10-9+/t21-,24-,25+,26-/m1/s1

SMILES Code: O=C([O-])CCCN[C@H](C1=CC=CC=C1)CN(C(N(CC2=C(C(F)(F)F)C=CC=C2F)C(C)=C3C4=CC=CC(OC)=C4F)=O)C3=O.[Na+]

Appearance: Solid powder

Purity: >95% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info: Elagolix is a novel, first-in-class oral gonadotropin-releasing hormone (GnRH) antagonist, which has recently completed a phase IIb study in endometriosis. In addition to endometriosis, elagolix will be evaluated for the treatment of uterine fibroids. . .

Instruction:

View handling instruction

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 653.57 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Shebley M, Polepally AR, Nader A, Ng JW, Winzenborg I, Klein CE, Noertersheuser P, Gibbs MA, Mostafa NM. Clinical Pharmacology of Elagolix: An Oral Gonadotropin-Releasing Hormone Receptor Antagonist for Endometriosis. Clin Pharmacokinet. 2019 Nov 21. doi: 10.1007/s40262-019-00840-7. [Epub ahead of print] Review. PubMed PMID: 31749075.

2: Neri M, Melis GB, Giancane E, Vallerino V, Pilloni M, Piras B, Loddo A, Paoletti AM, Mais V. Clinical Utility Of Elagolix As An Oral Treatment For Women With Uterine Fibroids: A Short Report On The Emerging Efficacy Data. Int J Womens Health. 2019 Oct 22;11:535-546. doi: 10.2147/IJWH.S185023. eCollection 2019. Review. PubMed PMID: 31695514; PubMed Central PMCID: PMC6815212.

3: LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012-. Available from http://www.ncbi.nlm.nih.gov/books/NBK548061/ PubMed PMID: 31643392.

4: Rolla E. Endometriosis: advances and controversies in classification, pathogenesis, diagnosis, and treatment. F1000Res. 2019 Apr 23;8. pii: F1000 Faculty Rev-529. doi: 10.12688/f1000research.14817.1. eCollection 2019. Review. PubMed PMID: 31069056; PubMed Central PMCID: PMC6480968.

5: Barra F, Scala C, Ferrero S. Elagolix sodium for the treatment of women with moderate to severe endometriosis-associated pain. Drugs Today (Barc). 2019 Apr;55(4):237-246. doi: 10.1358/dot.2019.55.4.2930713. Review. PubMed PMID: 31050692.

6: Farris M, Bastianelli C, Rosato E, Brosens I, Benagiano G. Uterine fibroids: an update on current and emerging medical treatment options. Ther Clin Risk Manag. 2019 Jan 23;15:157-178. doi: 10.2147/TCRM.S147318. eCollection 2019. Review. PubMed PMID: 30774352; PubMed Central PMCID: PMC6350833.

7: Elagolix (Orilissa)--an oral GnRH antagonist for endometriosis pain. Med Lett Drugs Ther. 2018 Sep 24;60(1556):158-160. Review. PubMed PMID: 30383729.

8: Drugs and Lactation Database (LactMed) [Internet]. Bethesda (MD): National Library of Medicine (US); 2006-. Available from http://www.ncbi.nlm.nih.gov/books/NBK525496/ PubMed PMID: 30222288.

9: Lamb YN. Elagolix: First Global Approval. Drugs. 2018 Sep;78(14):1501-1508. doi: 10.1007/s40265-018-0977-4. Review. Erratum in: Drugs. 2018 Nov 15;:. PubMed PMID: 30194661; PubMed Central PMCID: PMC6244606.

10: Ferrero S, Barra F, Leone Roberti Maggiore U. Current and Emerging Therapeutics for the Management of Endometriosis. Drugs. 2018 Jul;78(10):995-1012. doi: 10.1007/s40265-018-0928-0. Review. PubMed PMID: 29946962.

11: Taylor HS. Use of Elagolix in Gynaecology. J Obstet Gynaecol Can. 2018 Jul;40(7):931-934. doi: 10.1016/j.jogc.2018.01.004. Review. PubMed PMID: 29921430.

12: Barra F, Scala C, Mais V, Guerriero S, Ferrero S. Investigational drugs for the treatment of endometriosis, an update on recent developments. Expert Opin Investig Drugs. 2018 May;27(5):445-458. doi: 10.1080/13543784.2018.1471135. Epub 2018 May 17. Review. PubMed PMID: 29708812.

13: Legendre G, Delbos L, Hudon E, Chabbert-Buffet N, Geoffron S, Sauvan M, Fernandez H, Bouet PE, Descamps P. [New medical treatments for painful endometriosis: CNGOF-HAS Endometriosis Guidelines]. Gynecol Obstet Fertil Senol. 2018 Mar;46(3):256-263. doi: 10.1016/j.gofs.2018.02.009. Epub 2018 Mar 9. Review. French. PubMed PMID: 29530558.

14: Ciebiera M, Łukaszuk K, Męczekalski B, Ciebiera M, Wojtyła C, Słabuszewska-Jóźwiak A, Jakiel G. Alternative Oral Agents in Prophylaxis and Therapy of Uterine Fibroids-An Up-to-Date Review. Int J Mol Sci. 2017 Dec 1;18(12). pii: E2586. doi: 10.3390/ijms18122586. Review. PubMed PMID: 29194370; PubMed Central PMCID: PMC5751189.

15: Perricos A, Wenzl R. Efficacy of elagolix in the treatment of endometriosis. Expert Opin Pharmacother. 2017 Sep;18(13):1391-1397. doi: 10.1080/14656566.2017.1359258. Epub 2017 Jul 28. Review. PubMed PMID: 28737050.

16: Goenka L, George M, Sen M. A peek into the drug development scenario of endometriosis - A systematic review. Biomed Pharmacother. 2017 Jun;90:575-585. doi: 10.1016/j.biopha.2017.03.092. Epub 2017 Apr 10. Review. PubMed PMID: 28407578.

17: Alessandro P, Luigi N, Felice S, Maria PA, Benedetto MG, Stefano A. Research development of a new GnRH antagonist (Elagolix) for the treatment of endometriosis: a review of the literature. Arch Gynecol Obstet. 2017 Apr;295(4):827-832. doi: 10.1007/s00404-017-4328-6. Epub 2017 Mar 3. Review. PubMed PMID: 28255765.

18: Melis GB, Neri M, Corda V, Malune ME, Piras B, Pirarba S, Guerriero S, Orrù M, D'Alterio MN, Angioni S, Paoletti AM. Overview of elagolix for the treatment of endometriosis. Expert Opin Drug Metab Toxicol. 2016 May;12(5):581-8. doi: 10.1517/17425255.2016.1171316. Review. PubMed PMID: 27021205.

19: Soliman AM, Yang H, Du EX, Kelley C, Winkel C. The direct and indirect costs associated with endometriosis: a systematic literature review. Hum Reprod. 2016 Apr;31(4):712-22. doi: 10.1093/humrep/dev335. Epub 2016 Feb 6. Review. PubMed PMID: 26851604.

20: Leone Roberti Maggiore U, Ferrero S. An overview of early drug development for endometriosis. Expert Opin Investig Drugs. 2016;25(2):227-47. doi: 10.1517/13543784.2016.1126579. Epub 2015 Dec 19. Review. PubMed PMID: 26619754.

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