Linzagolix choline | CAS#1321816-57-2 | GnRH antagonist

MedKoo Cat#: 598947 | Name: Linzagolix choline

Description:

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

Linzagolix choline is a small-molecule, non-peptide, orally active gonadotropin-releasing hormone antagonist (GnRH antagonist) that potentially provides effective management of endometriosis-associated pain while mitigating bone mineral density loss and other adverse effects typically associated with currently approved treatments.

Chemical Structure

Linzagolix choline

CAS#1321816-57-2 (choline)

Theoretical Analysis

MedKoo Cat#: 598947

Name: Linzagolix choline

CAS#: 1321816-57-2 (choline)

Chemical Formula: C27H28F3N3O8S

Exact Mass: 611.1549

Molecular Weight: 611.58

Elemental Analysis: C, 53.03; H, 4.61; F, 9.32; N, 6.87; O, 20.93; S, 5.24

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.

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Related CAS #

935283-04-8 (anion) 1321816-57-2 (choline) 935283-04-8 (free acid)

Synonym

Linzagolix choline; OBE2109; OBE 2109; OBE-2109; KLH-2109; KLH 2109; KLH2109;

IUPAC/Chemical Name

2-hydroxy-N,N,N-trimethylethan-1-aminium 3-(5-((2,3-difluoro-6-methoxybenzyl)oxy)-2-fluoro-4-methoxyphenyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxylate

InChi Key

IAIVRTFCYOGNBW-UHFFFAOYSA-M

InChi Code

InChI=1S/C22H15F3N2O7S.C5H14NO/c1-32-14-4-3-10(23)18(25)9(14)7-34-16-6-13(11(24)5-15(16)33-2)27-20(28)17-12(26-22(27)31)8-35-19(17)21(29)30;1-6(2,3)4-5-7/h3-6,8H,7H2,1-2H3,(H,26,31)(H,29,30);7H,4-5H2,1-3H3/q;+1/p-1

SMILES Code

OCC[N+](C)(C)C.O=C(C1=C(C(N2C3=CC(OCC4=C(OC)C=CC(F)=C4F)=C(OC)C=C3F)=O)C(NC2=O)=CS1)[O-]

Appearance

Solid powder

Purity

>98% (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

Shelf Life

>3 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

2934.99.03.00

More Info

The gonadotropin-releasing hormone (GnRH) plays a key role in regulating estrogen levels, along with the levels of other reproductive hormones. GnRH is produced by the brain and binds to receptors on the pituitary gland. This stimulates the production of two hormones, follicle stimulating hormone (FSH) and luteinizing hormone (LH), which control the levels of reproductive hormones such as estrogen and progesterone. Among other roles in the body, estrogen and progesterone are essential to stimulating the growth and break down of the endometrium

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 611.58 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

1: Borini A, Coticchio G. Gonadotropin-releasing hormone antagonist linzagolix: possible treatment for assisted reproduction patients presenting with adenomyosis and endometriosis? Fertil Steril. 2020 Sep;114(3):517-518. doi: 10.1016/j.fertnstert.2020.06.003. Epub 2020 Aug 3. PMID: 32762949. 2: Donnez O, Donnez J. Gonadotropin-releasing hormone antagonist (linzagolix): a new therapy for uterine adenomyosis. Fertil Steril. 2020 Sep;114(3):640-645. doi: 10.1016/j.fertnstert.2020.04.017. Epub 2020 Jun 2. PMID: 32507315. 3: Donnez J, Taylor HS, Taylor RN, Akin MD, Tatarchuk TF, Wilk K, Gotteland JP, Lecomte V, Bestel E. Treatment of endometriosis-associated pain with linzagolix, an oral gonadotropin-releasing hormone-antagonist: a randomized clinical trial. Fertil Steril. 2020 Jul;114(1):44-55. doi: 10.1016/j.fertnstert.2020.02.114. Epub 2020 Jun 4. PMID: 32505383. 4: Pohl O, Marchand L, Bell D, Gotteland JP. Effects of combined GnRH receptor antagonist linzagolix and hormonal add-back therapy on vaginal bleeding-delayed add-back onset does not improve bleeding pattern. Reprod Sci. 2020 Apr;27(4):988-995. doi: 10.1007/s43032-020-00172-z. Epub 2020 Feb 25. PMID: 32100275.