1631164-24-3
1631164-24-3 結(jié)構(gòu)式
基本信息
中文別名
化合物 T10475化合物 BAY-784
英文別名
BAY-784BAY1214784
BAY784,BAY 784
(S)-N-((3-chloro-5-(trifluoromethyl)pyridin-2-yl)methyl)-2-cyclopropyl-1-((4-fluorophenyl)sulfonyl)-
Spiro[3H-indole-3,4'-[4H]thiopyran]-5-carboxamide, N-[[3-chloro-5-(trifluoromethyl)-2-pyridinyl]methyl]-2-cyclopropyl-1-[(4-fluorophenyl)sulfonyl]-1,2,2',3',5',6'-hexahydro-, 1',1'-dioxide, (2S)-
所屬類別
生物：拮抗劑物理化學(xué)性質(zhì)
密度1.60±0.1 g/cm3(Predicted)
儲(chǔ)存條件2-8°C
溶解度DMSO: 2mg/mL, clear
酸度系數(shù)(pKa)12.47±0.40(Predicted)
形態(tài)powder
顏色white to beige
旋光性 (optical activity)[α]/D -120 to -100°, c =0.5 in chloroform-d
常見問(wèn)題列表
生物活性
BAY-784 是一種促性腺激素釋放激素受體 (GnRH-R) 拮抗劑探針，對(duì)人和大鼠 GnRH-R 的 IC50 分別為 21 和 24 nM。靶點(diǎn)
IC50: 21 nM (human GnRH-R), 24 nM (rat GnRH-R)
體內(nèi)研究
BAY-784 (0.5, 3, 10, and 30 mg/kg; 24 hours; single p.o.) suppresses the plasma luteinizing hormone (LH) concentration in ovariectomized (OVX) rats in a dose-dependent manner.
| Animal Model: | OVX rats |
| Dosage: | 0.5, 3, 10, and 30 mg/kg (Pharmacokinetic Analysis) |
| Administration: | Single p.o. |
| Result: |
ED
50
=4.5 mg/kg (4/8 h).
The t 1/2 =13-17 h, 18 h, and 7 h for male Wistar rat, female beagle, and female cynomolgus, respectively. |