2-((1H-indol-3-yl)methyl)-9-(4-methoxypyrimidin-2-yl)-2,9-diazaspiro[5.5]undecan-1-one
IPSU
CAS: 1373765-19-5
Molecular Formula: C23H27N5O2
2-((1H-indol-3-yl)methyl)-9-(4-methoxypyrimidin-2-yl)-2,9-diazaspiro[5.5]undecan-1-one - Names and Identifiers
2-((1H-indol-3-yl)methyl)-9-(4-methoxypyrimidin-2-yl)-2,9-diazaspiro[5.5]undecan-1-one - Physico-chemical Properties
| Molecular Formula | C23H27N5O2 |
| Molar Mass | 405.49 |
| Density | 1.32±0.1 g/cm3(Predicted) |
| Boling Point | 702.0±70.0 °C(Predicted) |
| Solubility | DMSO: ≥ 30 mg/mL |
| pKa | 16.94±0.30(Predicted) |
| Storage Condition | -20℃ |
| In vitro study | 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. |
| In vivo study | 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 . |
2-((1H-indol-3-yl)methyl)-9-(4-methoxypyrimidin-2-yl)-2,9-diazaspiro[5.5]undecan-1-one - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.466 ml | 12.331 ml | 24.661 ml |
| 5 mM | 0.493 ml | 2.466 ml | 4.932 ml |
| 10 mM | 0.247 ml | 1.233 ml | 2.466 ml |
| 5 mM | 0.049 ml | 0.247 ml | 0.493 ml |
Last Update：2024-01-02 23:10:35
2-((1H-indol-3-yl)methyl)-9-(4-methoxypyrimidin-2-yl)-2,9-diazaspiro[5.5]undecan-1-one - Reference Information
| biological activity | IPSU is a selective, orally active and brain-permeable OX2R antagonist with a pKi value of 7.85. |
| Target | pKi: 7.85 (OX2R), 6.29 (OX1R) |
Last Update：2024-04-09 21:11:58
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CAS: 1373765-19-5
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CAS: 1373765-19-5
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
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