2471967-92-5
中文名稱
化合物 T10476
英文名稱
1,6-Naphthyridine-6(5H)-carboxamide, N-[2-(4-fluorophenoxy)-5-pyrimidinyl]-5-(4-fluorophenyl)-7,8-dihydro-, (5S)-
CAS
2471967-92-5
分子式
C25H19F2N5O2
分子量
459.45
MOL 文件
2471967-92-5.mol
2471967-92-5 結(jié)構(gòu)式
基本信息
中文別名
化合物 T10476 英文別名
BAY-8991,6-Naphthyridine-6(5H)-carboxamide, N-[2-(4-fluorophenoxy)-5-pyrimidinyl]-5-(4-fluorophenyl)-7,8-dihydro-, (5S)-
所屬類別
醫(yī)藥中間體物理化學(xué)性質(zhì)
密度1.397±0.06 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
酸度系數(shù)(pKa)12.52±0.40(Predicted)
形態(tài)Solid
顏色White to off-white
常見問題列表
生物活性
BAY-899 是一種口服有效和選擇性的促黃體生成激素受體 (LH-R) 拮抗劑，對(duì) hLH (人 LH) 和 rLH (大鼠 LH) 的 IC50 分別為 185 nM 和 46 nM。BAY-899 可以降低性激素水平。靶點(diǎn)
IC50: 185 nM (hLH) and 46nM (rLH)
體內(nèi)研究
BAY-899 (oral; 12.5 mg/kg/day; for 8 days) shows an efficiency to reduce serum estradiol levels in intact female rats.
BAY-899 (iv of 0.5 mg/kg or po of 2 mg/kg) has a t
1/2
of 11 hours and 12 hours for iv and po. And the C
max
is 0.97 kg/L and 0.24 kg/L for iv and po.
| Animal Model: | Intact female rats |
| Dosage: | 12.5 mg/kg |
| Administration: | Oral; for 8 days |
| Result: | Showed an efficiency to reduce serum estradiol levels. |
| Animal Model: | Female and male Wistar rats |
| Dosage: | 0.5 mg/kg of iv or 2 mg/kg of po |
| Administration: | Iv or po |
| Result: | Has t 1/2 s of 11 hours and 12 hours for iv and po. And the C max s are 0.97 kg/L and 0.24 kg/L for iv and po. |