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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.0%
- CAS. Nr.: 1373765-19-5
- Formel: C23H27N5O2
- Molecular Weight:405.49
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) IPSU
MoreAlle Orexin Receptor (OX Receptor) Isoform-spezifische Produkte anzeigen
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Biologische Aktivität
pKi: 7.85 (OX2R), 6.29 (OX1R)[1]
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 1373765-19-5
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Appearance Solid
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Molecular Weight 405.49
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
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
Lösungsmittel & Löslichkeit
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Protokoll
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.
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.
Reinheit & Dokumentation
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Data Sheet (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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Handling Instructions (2659 KB)
Verweise
[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 |
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| 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 Related Classifications
HY-13796 Related Classifications
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