Uses
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].
in vivo
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].
| Animal Model: | Intact female rats[1] |
| Dosage: | 4.5, 9, 18, 36, 72 mg/kg |
| Administration: | Oral; for 8 days |
| Result: | Dosedependently lowered serum estradiol levels in proestrus.
|
| Animal Model: | Female and male Wistar rats[1] |
| Dosage: | 0.5 mg/kg of iv or 2 mg/kg of po |
| Administration: | Iv or po |
| Result: | 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.
|
References
[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. DOI:
10.1021/acs.jmedchem.9b01382
![1,6-Naphthyridine-6(5H)-carboxamide, 5-(4-chlorophenyl)-N-[4-(4-fluorophenoxy)phenyl]-7,8-dihydro-, (5S)- Structure](https://www.chemicalbook.com/CAS/20210111/GIF/2471978-97-7.gif)
