BAY-298 是一种口服有效和选择性的促黄体生成激素受体 (LH-R) 拮抗剂，对 hLH (人 LH)，rLH (大鼠 LH)和 cLH (食蟹猴LH) 的 IC50 分别为 96 nM，23 nM 和 78 nM。BAY-298 可以降低性激素水平。
货号:ajcx34556
CAS:2471978-97-7
分子式:C27H21ClFN3O2
分子量：473.93
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

BAY-298 is an orally active and selective luteinizing hormone receptor (LH-R) antagonist with IC50s of 96 nM, 23 nM and 78 nM for hLH (human LH) and rLH (rat LH) and cLH (cynomolgus monkey LH), respectively. BAY-298 can reduce sex hormone levels[1].

BAY-298 (oral; 4.5-72 mg/kg/day; for 8 days) dosedependently loweres serum estradiol levels in proestrus[1]. BAY-298 (iv of 0.5 mg/kg or po of 2 mg/kg) has t1/2s of 31 hours and 33 hours for iv and po. And the Cmaxs are 0.28 kg/L and 0.066 kg/L for iv and po[1].

[1]. Wortmann L, et al. Discovery of BAY-298 and BAY-899: Tetrahydro-1,6-naphthyridine-Based, Potent and Selective Antagonists of the Luteinizing Hormone Receptor Which Reduce Sex Hormone Levels In Vivo. J Med Chem. 2019 Oct 31.