| Identification | Back Directory | [Name]
Linzagolix | [CAS]
935283-04-8 | [Synonyms]
Linzagolix
Thieno[3,4-d]pyrimidine-5-carboxylic acid, 3-[5-[(2,3-difluoro-6-methoxyphenyl)methoxy]-2-fluoro-4-methoxyphenyl]-1,2,3,4-tetrahydro-2,4-dioxo- | [Molecular Formula]
C22H15F3N2O7S | [MOL File]
935283-04-8.mol | [Molecular Weight]
508.42 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 125 mg/mL (245.86 mM; Need ultrasonic) | [form ]
Solid | [color ]
White to light brown | [InChIKey]
BMAAMIIYNNPHAB-UHFFFAOYSA-N | [SMILES]
C1(=O)N(C2=CC(OCC3=C(OC)C=CC(F)=C3F)=C(OC)C=C2F)C(=O)C2=C(C(O)=O)SC=C2N1 |
| Hazard Information | Back Directory | [Uses]
Linzagolix (KLH-2109; OBE-2109) is a potent, non-peptide, and orally active GnRH antagonist. Linzagolix can be used for uterine fibroids, endometriosis, adenomyosis research[1][2][3]. | [in vivo]
Linzagolix (50 mg/kg) reduces cyst volume in a rat model of endometriosis[1].
Lindagolix reduces serum luteinizing hormone and testosterone levels in male rats and dogs with normal or BPH models[2]. | Animal Model: | Endometriosis model rat[1] | | Dosage: | 50 mg/kg | | Administration: | | | Result: | Reduced cyst volume. |
| [References]
[1] Motohiro Tezuka, 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. 2023 Jul;50(7):610-617. DOI:10.1111/1440-1681.13778
[2] Motohiro Tezuka, et al. Suppression of hypothalamic-pituitary-gonadal function by linzagolix in benign prostatic hyperplasia and polycystic ovary syndrome animal models. Clin Exp Pharmacol Physiol. 2023 Nov;50(11):914-923. DOI:10.1111/1440-1681.13817
[3] Susan Dababou, et al. Linzagolix: a new GnRH-antagonist under investigation for the treatment of endometriosis and uterine myomas. Expert Opin Investig Drugs. 2021 Sep;30(9):903-911. DOI:10.1080/13543784.2021.1957830 |
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