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

Chemical Structure : Linzagolix

CAS No.: 935283-04-8

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

货号: 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).

规格	价格	库存
5 mg	￥780	In stock
10 mg	￥1180	In stock
25 mg	￥2180	In stock
50 mg	￥3580	In stock
100 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	508.424
分子式	C22H15F3N2O7S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
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

参考文献

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

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

生物&药学活性

物理化学性质&存储条件

参考文献

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

生物&药学活性

物理化学性质&存储条件

参考文献

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