Linzagolix (KLH-2109, OBE-2109) | GnRH antagonist

Chemical Structure : Linzagolix

CAS No.: 935283-04-8

Linzagolix (KLH-2109, OBE-2109, KLH2109, OBE2109)

Catalog No.: PC-61385Not For Human Use, Lab Use Only.

Linzagolix (KLH-2109, OBE-2109) is a potent, non-peptide, and orally active gonadotrophin releasing hormone (GnRH) antagonist, inhibits GnRH-stimulated Ca2+ flux with IC50 of 36.7 nM (human GnRH receptor).

Packing	Price	Stock
5 mg	$78	In stock
10 mg	$118	In stock
25 mg	$218	In stock
50 mg	$358	In stock
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Biological Activity

Linzagolix (KLH-2109, OBE-2109) is a potent, non-peptide, and orally active gonadotrophin releasing hormone (GnRH) antagonist, inhibits GnRH-stimulated Ca2+ flux with IC50 of 36.7 nM (human GnRH receptor).

Linzagolix shows 12-fold lower potency for the monkey GnRH receptor.

Linzagolix selectively binds to the GnRH receptor and inhibits GnRH-stimulated signalling, in a manner comparable to cetrorelix, a peptide GnRH antagonist.

Linzagolix suppressed the serum luteinizing hormone concentration at doses over 1 mg/kg in ovariectomized monkeys.

Linzagolix suppressed hormone surges and ceased or prolonged menstrual cycles in intact female monkeys.

Physicochemical Properties

M.Wt	508.424
Formula	C22H15F3N2O7S
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	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

References

1. Tezuka M, et al. Clin Exp Pharmacol Physiol. 2022 Oct;49(10):1082-1093.

Linzagolix (KLH-2109, OBE-2109, KLH2109, OBE2109)

Biological Activity

Physicochemical Properties

References

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