BAY-899

• CAT Number: I017731
• CAS Number: 2471967-92-5
• Molecular Formula: C25H19F2N5O2
• Molecular Weight: 459.45
• Purity: ≥95%
• Synonyms: (5S)-N-[2-(4-fluorophenoxy)pyrimidin-5-yl]-5-(4-fluorophenyl)-7,8-dihydro-5H-1,6-naphthyridine-6-carboxamide
• InChI: InChI=1S/C25H19F2N5O2/c26-17-5-3-16(4-6-17)23-21-2-1-12-28-22(21)11-13-32(23)25(33)31-19-14-29-24(30-15-19)34-20-9-7-18(27)8-10-20/h1-10,12,14-15,23H,11,13H2,(H,31,33)/t23-/m0/s1
• InChIKey: VKQBTIMLSDGNLG-QHCPKHFHSA-N
• SMILES: C1CN(C(C2=C1N=CC=C2)C3=CC=C(C=C3)F)C(=O)NC4=CN=C(N=C4)OC5=CC=C(C=C5)F

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].
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].

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.
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