1,6-Naphthyridine-6(5H)-carboxamide, N-[2-(4-fluorophenoxy)-5-pyrimidinyl]-5-(4-fluorophenyl)-7,8-dihydro-, (5S)- manufacturers
- BAY-899
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- $4700.00
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2026-05-21
- CAS:2471967-92-5
- Purity:
- Supply Ability: 10g
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| | 1,6-Naphthyridine-6(5H)-carboxamide, N-[2-(4-fluorophenoxy)-5-pyrimidinyl]-5-(4-fluorophenyl)-7,8-dihydro-, (5S)- Basic information |
| Product Name: | 1,6-Naphthyridine-6(5H)-carboxamide, N-[2-(4-fluorophenoxy)-5-pyrimidinyl]-5-(4-fluorophenyl)-7,8-dihydro-, (5S)- | | Synonyms: | 1,6-Naphthyridine-6(5H)-carboxamide, N-[2-(4-fluorophenoxy)-5-pyrimidinyl]-5-(4-fluorophenyl)-7,8-dihydro-, (5S)-;(5S)-N-[2-(4-fluorophenoxy)pyrimidin-5-yl]-5-(4-fluorophenyl)-5,6,7,8-tetrahydro-1,6-naphthyridine-6-carboxamide;BAY-899 | | CAS: | 2471967-92-5 | | MF: | C25H19F2N5O2 | | MW: | 459.45 | | EINECS: | | | Product Categories: | APIs | | Mol File: | 2471967-92-5.mol | ![1,6-Naphthyridine-6(5H)-carboxamide, N-[2-(4-fluorophenoxy)-5-pyrimidinyl]-5-(4-fluorophenyl)-7,8-dihydro-, (5S)- Structure](CAS/20210111/GIF/2471967-92-5.gif) |
| | 1,6-Naphthyridine-6(5H)-carboxamide, N-[2-(4-fluorophenoxy)-5-pyrimidinyl]-5-(4-fluorophenyl)-7,8-dihydro-, (5S)- Chemical Properties |
| density | 1.397±0.06 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMSO: 1mg/mL, clear | | pka | 12.52±0.40(Predicted) | | form | Solid | | color | White to off-white | | Optical Rotation | [α]/D 165 to 195°, c =1 in chloroform-d | | InChIKey | VKQBTIMLSDGNLG-QHCPKHFHSA-N | | SMILES | O=C(N1[C@@H](C2=CC=C(F)C=C2)C3=C(N=CC=C3)CC1)NC4=CN=C(OC5=CC=C(F)C=C5)N=C4 |
| WGK Germany | WGK 3 | | Storage Class | 11 - Combustible Solids |
| | 1,6-Naphthyridine-6(5H)-carboxamide, N-[2-(4-fluorophenoxy)-5-pyrimidinyl]-5-(4-fluorophenyl)-7,8-dihydro-, (5S)- Usage And Synthesis |
| Uses | 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]. | | Biological Activity | BAY-899 is an orally available, potent and selective antagonist of the human luteinizing hormone receptor (hLH-R) th at reduces sex hormone levels in several animal models. BAY-899 likely binds to a putative rhodopsin-like binding cavity located within the 7-transmembrane region of the hLH-receptor. | | 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: | Intact female rats[1] | | Dosage: | 12.5 mg/kg | | Administration: | Oral; for 8 days | | Result: | Showed an efficiency to reduce serum estradiol levels.
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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 11 hours and 12 hours for iv and po. And the Cmaxs are 0.97 kg/L and 0.24 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 |
| | 1,6-Naphthyridine-6(5H)-carboxamide, N-[2-(4-fluorophenoxy)-5-pyrimidinyl]-5-(4-fluorophenyl)-7,8-dihydro-, (5S)- Preparation Products And Raw materials |
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