Linzagolix
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MedKoo CAT#: 561854

CAS#: 935283-04-8 (free)

Description: 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

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Linzagolix
CAS# 935283-04-8 (free)

Theoretical Analysis

MedKoo Cat#: 561854
Name: Linzagolix
CAS#: 935283-04-8 (free)
Chemical Formula: C22H15F3N2O7S
Exact Mass: 508.06
Molecular Weight: 508.420
Elemental Analysis: C, 51.97; H, 2.97; F, 11.21; N, 5.51; O, 22.03; S, 6.31

Price and Availability

Size Price Availability Quantity
10mg USD 350 2 Weeks
25mg USD 650 2 Weeks
50mg USD 1050 2 Weeks
100mg USD 1850 2 Weeks
200mg USD 2950 2 Weeks
Bulk inquiry

Related CAS #: 935283-04-8 (free)   1321816-57-2 (choline)    

Synonym: Linzagolix; OBE2109; OBE 2109; OBE-2109; KLH-2109; KLH 2109; KLH2109;

IUPAC/Chemical Name: 3-{5-[(2,3-difluoro-6-methoxyphenyl)methoxy]-2-fluoro-4-methoxyphenyl}-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxylic acid

InChi Key: BMAAMIIYNNPHAB-UHFFFAOYSA-N

InChi Code: InChI=1S/C22H15F3N2O7S/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/h3-6,8H,7H2,1-2H3,(H,26,31)(H,29,30)

SMILES Code: 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: >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: 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

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 508.42 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.

Recalculate based on batch purity %
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: 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.