2471978-97-7
中文名称
化合物 T10469
英文名称
1,6-Naphthyridine-6(5H)-carboxamide, 5-(4-chlorophenyl)-N-[4-(4-fluorophenoxy)phenyl]-7,8-dihydro-, (5S)-
CAS
2471978-97-7
分子式
C27H21ClFN3O2
分子量
473.93
MOL 文件
2471978-97-7.mol
2471978-97-7 结构式
基本信息
中文别名
化合物 T10469 英文别名
BAY-298PF-06873600 (free base)
1,6-Naphthyridine-6(5H)-carboxamide, 5-(4-chlorophenyl)-N-[4-(4-fluorophenoxy)phenyl]-7,8-dihydro-, (5S)-
物理化学性质
沸点653.6±55.0 °C(Predicted)
密度1.353±0.06 g/cm3(Predicted)
酸度系数(pKa)12.36±0.70(Predicted)
形态Solid
颜色Off-white to light yellow
常见问题列表
生物活性
BAY-298 是一种口服有效和选择性的促黄体生成激素受体 (LH-R) 拮抗剂，对 hLH (人 LH)，rLH (大鼠 LH)和 cLH (食蟹猴LH) 的 IC50 分别为 96 nM，23 nM 和 78 nM。BAY-298 可以降低性激素水平。靶点
IC50: 185 nM (hLH), 46nM (rLH) and 78 nM (cLH)
体内研究
BAY-298 (oral; 4.5-72 mg/kg/day; for 8 days) dosedependently loweres serum estradiol levels in proestrus.
BAY-298 (iv of 0.5 mg/kg or po of 2 mg/kg) has t
1/2
s of 31 hours and 33 hours for iv and po. And the C
max
s are 0.28 kg/L and 0.066 kg/L for iv and po.
| Animal Model: | Intact female rats |
| Dosage: | 4.5, 9, 18, 36, 72 mg/kg |
| Administration: | Oral; for 8 days |
| Result: | Dosedependently lowered serum estradiol levels in proestrus. |
| 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 31 hours and 33 hours for iv and po. And the C max s are 0.28 kg/L and 0.066 kg/L for iv and po. |