2,9-Diazaspiro[5.5]undecan-1-one, 2-(1H-indol-3-ylMethyl)-9-(4-Methoxy-2-pyriMidinyl)-
中文名称 | 2,9-Diazaspiro[5.5]undecan-1-one, 2-(1H-indol-3-ylMethyl)-9-(4-Methoxy-2-pyriMidinyl)- |
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中文同义词 | 化合物IPSU |
英文名称 | 2,9-Diazaspiro[5.5]undecan-1-one, 2-(1H-indol-3-ylMethyl)-9-(4-Methoxy-2-pyriMidinyl)- |
英文同义词 | 2,9-Diazaspiro[5.5]undecan-1-one, 2-(1H-indol-3-ylMethyl)-9-(4-Methoxy-2-pyriMidinyl)-;IPSU;2-(1H-Indol-3-ylmethyl)-9-(4-methoxy-2-pyrimidinyl)-2,9-diazaspiro[5.5]undecan-1-one;2-((1H-indol-3-yl)methyl)-9-(4-methoxypyrimidin-2-yl)-2,9-diazaspiro[5.5]undecan-1-one;inhibit,HCRT Receptor,Hypocretin Receptor,IPSU,Orexin Receptor (OX Receptor),Inhibitor |
CAS号 | 1373765-19-5 |
分子式 | C23H27N5O2 |
分子量 | 405.49 |
EINECS号 | 604-604-1 |
相关类别 | |
Mol文件 | 1373765-19-5.mol |
结构式 |
2,9-Diazaspiro[5.5]undecan-1-one, 2-(1H-indol-3-ylMethyl)-9-(4-Methoxy-2-pyriMidinyl)- 性质
沸点 | 702.0±70.0 °C(Predicted) |
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密度 | 1.32±0.1 g/cm3(Predicted) |
储存条件 | Store at -20°C |
溶解度 | DMSO:30.0(最大浓度 mg/mL);73.98(最大浓度 mM) |
形态 | 结晶固体 |
酸度系数(pKa) | 16.94±0.30(Predicted) |
pKi: 7.85 (OX2R), 6.29 (OX1R)
Orexin receptor antagonists represent attractive targets for the development of drugs for the treatment of insomnia. IPSU binds rapidly and reaches equilibrium very quickly in binding and/or functional assays.
IPSU has low blood clearance, shows high maximal blood exposure and AUC after oral dosing. It exhibits an acceptable absolute oral bioavailability and a brain/blood concentration ratio that indicated favorable brain penetration. IPSU increases sleep when dosed during the mouse active phase (lights off); IPSU induces sleep primarily by increasing NREM sleep. IPSU shows a fast onset of action, with a clear increase in total sleep time during the first hour afterdosing. The effect lasts 4-5 h, after which time the total sleep time per hour is the same as on vehicle day .
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/04/30 | HY-13796 | IPSU | 1 mg | 420元 | |
2024/04/30 | HY-13796 | 2,9-Diazaspiro[5.5]undecan-1-one, 2-(1H-indol-3-ylMethyl)-9-(4-Methoxy-2-pyriMidinyl)- IPSU | 1373765-19-5 | 5mg | 1100元 |