Masupirdine mesylate
Based on 1 Customer Validation
Masupirdine mesylate (SUVN-502 mesylate) is a potent, selective, orally active, and brain-penetrating 5-HT6 receptor antagonist (Ki of 2.04 nM for human 5-HT6 receptor). Masupirdine mesylate has pro-cognitive effects on all stages of cognition (acquisition, consolidation, and retention), and can reverse Scopolamine (HY-N0296), MK-801 (HY-15084B)-induced and aging-related memory deficits. Masupirdine mesylate can be used in the research of Alzheimer's disease.
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- Pureté : 99.62%
- CAS No.: 1791396-46-7
- Formule: C23H32BrN3O9S3
- Masse moléculaire:670.61
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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
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Activité biologique
Description
IC50 & Target
[1]|
5-HT6 Receptor 2.04 nM (Ki) |
5-HT2A Receptor |
5-HT6 Receptor |
In Vitro
Masupirdine (10 μM) mesylate shows no agonist or partial agonist effects on luciferase activity but blocks serotonin-induced luciferase activity in the 5-HT6 receptor functional assay using CHO-K1 cells stably expressing human 5-HT6 receptor and CRE-Luc reporter gene[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1791396-46-7
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Appearance Solid
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Masse moléculaire 670.61
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Formule C23H32BrN3O9S3
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Color Pale purple to purple
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SMILES
CS(=O)(O)=O.O=S(N1C2=CC=C(OC)C=C2C(CN3CCN(C)CC3)=C1)(C(C=CC=C4)=C4Br)=O.CS(=O)(O)=O
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Synonyms
SUVN-502 mesylate
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvant et solubilité
In Vitro:
DMSO : 25 mg/mL (37.28 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (280 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]. Nirogi R, et al. Discovery and Development of 1-[(2-Bromophenyl)sulfonyl]-5-methoxy-3-[(4-methyl-1-piperazinyl)methyl]-1H-indole Dimesylate Monohydrate (SUVN-502): A Novel, Potent, Selective and Orally Active Serotonin 6 (5-HT6) Receptor Antagonist for Potential Treatment of Alzheimer's Disease. J Med Chem. 2017 Mar 9;60(5):1843-1859. [Content Brief]
[2]. Nirogi R, et al. SUVN-502, a novel, potent, pure, and orally active 5-HT6 receptor antagonist: pharmacological, behavioral, and neurochemical characterization. Behav Pharmacol. 2019 Feb;30(1):16-35. [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 | 1 mM | 1.4912 mL | 7.4559 mL | 14.9118 mL | 37.2795 mL |
| 5 mM | 0.2982 mL | 1.4912 mL | 2.9824 mL | 7.4559 mL | |
| 10 mM | 0.1491 mL | 0.7456 mL | 1.4912 mL | 3.7279 mL | |
| 15 mM | 0.0994 mL | 0.4971 mL | 0.9941 mL | 2.4853 mL | |
| 20 mM | 0.0746 mL | 0.3728 mL | 0.7456 mL | 1.8640 mL | |
| 25 mM | 0.0596 mL | 0.2982 mL | 0.5965 mL | 1.4912 mL | |
| 30 mM | 0.0497 mL | 0.2485 mL | 0.4971 mL | 1.2426 mL |
Masupirdine mesylate Related Classifications
HY-109118A Related Classifications
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