Bioactivity | BAY-899 is an orally active and selective luteinizing hormone receptor (LH-R) antagonist with IC50s of 185 nM and 46nM for hLH (human LH) and rLH (rat LH), respectively. BAY-899 can reduce sex hormone levels[1]. | ||||||||||||
Target | IC50: 185 nM (hLH) and 46nM (rLH) | ||||||||||||
In Vivo | BAY-899 (oral; 12.5 mg/kg/day; for 8 days) shows an efficiency to reduce serum estradiol levels in intact female rats[1]. BAY-899 (iv of 0.5 mg/kg or po of 2 mg/kg) has a t1/2 of 11 hours and 12 hours for iv and po. And the Cmax is 0.97 kg/L and 0.24 kg/L for iv and po[1]. Animal Model: | ||||||||||||
Name | BAY-899 | ||||||||||||
CAS | 2471967-92-5 | ||||||||||||
Formula | C25H19F2N5O2 | ||||||||||||
Molar Mass | 459.45 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [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. |