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.
For research use only. We do not sell to patients.
- Purity: 99.62%
- CAS No.: 1791396-46-7
- Formula: C23H32BrN3O9S3
- Molecular Weight:670.61
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
All 5-HT Receptor Isoforms
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Biological Activity
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5-HT6 Receptor 2.04 nM (Ki) |
5-HT2A Receptor |
5-HT6 Receptor |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| 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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Molecular Weight 670.61
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
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)
Purity & Documentation
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Data Sheet (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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Handling Instructions (2659 KB)
References
[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 |