| Identification | Back Directory | [Name]
1,6-Naphthyridine-6(5H)-carboxamide, 5-(4-chlorophenyl)-N-[4-(4-fluorophenoxy)phenyl]-7,8-dihydro-, (5S)- | [CAS]
2471978-97-7 | [Synonyms]
BAY-298
1,6-Naphthyridine-6(5H)-carboxamide, 5-(4-chlorophenyl)-N-[4-(4-fluorophenoxy)phenyl]-7,8-dihydro-, (5S)- | [Molecular Formula]
C27H21ClFN3O2 | [MOL File]
2471978-97-7.mol | [Molecular Weight]
473.93 |
| Chemical Properties | Back Directory | [Boiling point ]
653.6±55.0 °C(Predicted) | [density ]
1.353±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
12.36±0.70(Predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [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.
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| 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.
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| [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 |
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