A GnRH receptor antagonist
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Linzagolix

Item No. 39654

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-[5-[(2,3-difluoro-6-methoxyphenyl)methoxy]-2-fluoro-4-methoxyphenyl]-1,2,3,4-tetrahydro-2,4-dioxo-thieno[3,4-d]pyrimidine-5-carboxylic acid
CAS Number
935283-04-8
Synonyms
  • KLH-2109
  • OBE-2109
Molecular Formula
C22H15F3N2O7S
Formula Weight
508.4
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: SolubleDMSO: Soluble
SMILES
O=C(C(SC=C1NC(N2C3=C(F)C=C(OC)C(OCC4=C(C(F)=CC=C4OC)F)=C3)=O)=C1C2=O)O
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)
InChi Key
BMAAMIIYNNPHAB-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $39

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    5 mg

    $164

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    10 mg

    $308

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    25 mg

    $626

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    Product Description

    Linzagolix is a nonpeptide gonadotropin-releasing hormone (GnRH) receptor antagonist (IC50 = 36.7 nM for the human receptor).1 Unlike the peptide GnRH receptor antagonist cetrorelix (Item No. 23910), linzagolix (10 µM) does not induce histamine release in isolated rat peritoneal mast cells.2 Linzagolix (25 and 50 mg/kg) suppresses the menstrual cycle in normal cynomolgus monkeys.1 It decreases serum luteinizing hormone (LH) levels in ovariectomized cynomolgus monkeys when administered at doses ranging from 1 to 100 mg/kg. Linzagolix (50-200 mg/kg, p.o.) decreases cyst volume in a rat model of endometriosis induced by autotransplantation of endometrial tissue into the renal subcapsular space.2 Formulations containing linzagolix have been used in the treatment of uterine fibroids.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Tezuka, M., Tamai, Y., Kuramochi, Y., et al. Pharmacological characterization of linzagolix, a novel, orally active, non-peptide antagonist of gonadotropin-releasing hormone receptors. Clin. Exp. Pharmacol. Physiol. 49(10), 1082-1093 (2022).

    2. Tezuka, M., Tsuchioka, K., Kobayashi, K., et al. Suppressive effects of linzagolix, a novel non-peptide antagonist of gonadotropin-releasing hormone receptors, in experimental endometriosis model rats. Clin. Exp. Pharmacol. Physiol. 50(7), 610-617 (2023).