SKF 83959 hydrobromide
Based on 1 publication(s) in Google Scholar
SKF83959 hydrobromide is a potent and selective dopamine D1-like receptor partial agonist. SKF83959 hydrobromide Ki values for rat D1, D5, D2 and D3 receptors are 1.18, 7.56, 920 and 399 nM, respectively. SKF83959 hydrobromide is a potent allosteric modulator of sigma (σ)-1 receptor. SKF83959 hydrobromide belongs to benzazepine family and has improvements on cognitive dysfunction. SKF83959 hydrobromide can be used for the research of Alzheimer's disease and depression.
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- Pureté : 99.86%
- CAS No.: 67287-95-0
- Formule: C18H21BrClNO2
- Masse moléculaire:398.72
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Stockage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) SKF 83959 hydrobromide
MoreVoir tous les produits spécifiques à Isoform Dopamine Receptor
MoreVoir tous les produits spécifiques à Isoform Sigma Receptor
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Activité biologique
Description
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D1 Receptor 1.18 nM (Ki) |
D5 Receptor 7.56 nM (Ki) |
D2 Receptor 920 nM (Ki) |
D3 Receptor 399 nM (Ki) |
sigma (σ)-1 |
In Vitro
SKF83959 hydrobromide (10~250 μM) stimulates PIP2 hydrolysis in membranes. SKF83959 hydrobromide (0.1~10 μM; PC12 cell) changes the EC50 value of SKF81297 from 0.5 nM in control tissue to 31.6 nM, 251.2 nM and 631.0 nM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
SKF83959 hydrobromide (1 mg/kg; i.p.; 30 minutes) induced memory enhancing effects are prevented by brain-derived neurotrophic factor system blockade[1].
SKF83959 hydrobromide has anti-amnesic activities and restores the scopolamine-decreased BDNF signaling pathway in the hippocampus in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male ICR male mice (8 weeks)[1]
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Dosage:0.5 and 1 mg/kg
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Administration:I.p.; 1 hour
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Result:Reversed the scopolamine-induced cognitive impairments in the passive avoidance task and Y-Maze test.
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Animal Model:Male ICR male mice (8 weeks)[1]
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Dosage:1 mg/kg
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Administration:I.p.; 30 minutes
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Result:The memory enhancing effects were prevented by BDNF system blockade.
Chemical Information
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CAS No. 67287-95-0
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Appearance Solid
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Masse moléculaire 398.72
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Formule C18H21BrClNO2
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Color White to light brown
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SMILES
OC1=C(O)C=C2C(C3=CC=CC(C)=C3)CN(C)CCC2=C1Cl.[H]Br
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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Nature
2023 Dec;624(7992):672-681. PMID: 37935376
Solvant et solubilité
In Vitro:
DMSO : 20 mg/mL (50.16 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
DMF : 20 mg/mL (50.16 mM; Need ultrasonic and warming)
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocole
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Alzheimer’s Disease Modeling
Alzheimer’s Disease (AD) is a neurodegenerative disorder characterized by a progressive decline in cognitive functions and loss of specific types of neurons and synapses. Alzheimer's symptoms can be simulated in mice by injecting drugs (such as Aβ) or genetically modified.
Pureté et documentation
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Fiche technique (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Sheng G, et al. SKF83959 Has Protective Effects in the Scopolamine Model of Dementia. Biol Pharm Bull. 2018;41(3):427-434. [Content Brief]
[2]. Jin LQ, et al. SKF83959 selectively regulates phosphatidylinositol-linked D1 dopamine receptors in rat brain. J Neurochem. 2003;85(2):378-386. [Content Brief]
[3]. Neumeyer JL, et al. Receptor affinities of dopamine D1 receptor-selective novel phenylbenzazepines. Eur J Pharmacol. 2003;474(2-3):137-140. [Content Brief]
[4]. Guo L, et al. SKF83959 is a potent allosteric modulator of sigma-1 receptor. Mol Pharmacol. 2013;83(3):577-586. [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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / DMF | 1 mM | 2.5080 mL | 12.5401 mL | 25.0803 mL | 62.7006 mL |
| 5 mM | 0.5016 mL | 2.5080 mL | 5.0161 mL | 12.5401 mL | |
| 10 mM | 0.2508 mL | 1.2540 mL | 2.5080 mL | 6.2701 mL | |
| 15 mM | 0.1672 mL | 0.8360 mL | 1.6720 mL | 4.1800 mL | |
| 20 mM | 0.1254 mL | 0.6270 mL | 1.2540 mL | 3.1350 mL | |
| 25 mM | 0.1003 mL | 0.5016 mL | 1.0032 mL | 2.5080 mL | |
| 30 mM | 0.0836 mL | 0.4180 mL | 0.8360 mL | 2.0900 mL | |
| 40 mM | 0.0627 mL | 0.3135 mL | 0.6270 mL | 1.5675 mL | |
| 50 mM | 0.0502 mL | 0.2508 mL | 0.5016 mL | 1.2540 mL |
SKF 83959 hydrobromide Related Classifications
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