IPSU
Based on 1 publication(s) in Google Scholar
IPSU is a selective, orally available and brain penetrant OX2R antagonist with a pKi of 7.85.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.0%
- CAS 番号: 1373765-19-5
- 分子式: C23H27N5O2
- 分子量:405.49
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 IPSU
MoreOrexin Receptor (OX Receptor) アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
IC50 & Target
pKi: 7.85 (OX2R), 6.29 (OX1R)[1]
体外実験
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[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 1373765-19-5
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性状 Solid
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分子量 405.49
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分子式 C23H27N5O2
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Color White to off-white
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SMILES
COC1=CC=NC(N(CC2)CCC2(C3=O)CCCN3CC4=CNC5=CC=CC=C54)=N1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Molecules
2020 Feb 25;25(5):1018. PMID: 32106419
溶剤 & 溶解度
体外:
DMSO : ≥ 30 mg/mL (73.98 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
プロトコル
Kinase Assay[2]
Competition experiments are performed with a single concentration of radioligand and six concentrations of competitor (unlabeled ligands; BBAC, almorexant, SB-649868, suvorexant, filorexant or IPSU). 4.6 nM [3H]-BBAC is added simultaneously with various concentrations of unlabeled ligand (0.1 nM-10 μM) to membranes (150 μL/well) in 50 μL/well of assay buffer with a total volume of 250 μL/well. The amount of [3H]-BBAC bound to receptors is determined at room temperature at different time points (ranging from 15 min to 4 h) and terminated by rapid vacuum filtration and liquid scintillation counting[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration[1]
Mice: Freely moving C57Bl/6 mice with chronically implanted electrodes are well abituated to the experiment boxes and had access to food and ater ad libitum. The test compounds (IPSU) or vehicle are administered per os as a suspension in 0.5% methylcellulose immediately prior to lights off and start of recording. Movement is recorded using infrared sensors in the roof of the box. EEG/EMG signals and motility data are used to score 10 s epochs into wake, NREM sleep, and REM sleep. Each animal served as its own control by application and recording of vehicle the day before compound (IPSU) dosing[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (275 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Betschart C, et al. Identification of a novel series of orexin receptor antagonists with a distinct effect on sleeparchitecture for the treatment of insomnia. J Med Chem. 2013 Oct 10;56(19):7590-607. [Content Brief]
[2]. Callander GE, et al. Kinetic properties of "dual" orexin receptor antagonists at OX1R and OX2R orexin receptors. Front Neurosci. 2013 Dec 3;7:230. [Content Brief]
[3]. Hoyer D, et al. Distinct effects of IPSU and suvorexant on mouse sleep architecture. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4662 mL | 12.3308 mL | 24.6615 mL | 61.6538 mL |
| 5 mM | 0.4932 mL | 2.4662 mL | 4.9323 mL | 12.3308 mL | |
| 10 mM | 0.2466 mL | 1.2331 mL | 2.4662 mL | 6.1654 mL | |
| 15 mM | 0.1644 mL | 0.8221 mL | 1.6441 mL | 4.1103 mL | |
| 20 mM | 0.1233 mL | 0.6165 mL | 1.2331 mL | 3.0827 mL | |
| 25 mM | 0.0986 mL | 0.4932 mL | 0.9865 mL | 2.4662 mL | |
| 30 mM | 0.0822 mL | 0.4110 mL | 0.8221 mL | 2.0551 mL | |
| 40 mM | 0.0617 mL | 0.3083 mL | 0.6165 mL | 1.5413 mL | |
| 50 mM | 0.0493 mL | 0.2466 mL | 0.4932 mL | 1.2331 mL | |
| 60 mM | 0.0411 mL | 0.2055 mL | 0.4110 mL | 1.0276 mL |
IPSU 関連分類
HY-13796 関連分類
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